Ligand source activities (1 row/activity)



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

 p-value
(-log)		 Activity
Type		 Activity
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Description		 Source

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122194229 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
1324 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
16197727 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
4836 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
CHEMBL3629347 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
CHEMBL441738 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
DB04931 621 23 None -4 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm101425m
CHEMBL2371966 485796 0 None 912 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1015 12 8 9 2.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
118722937 235161 0 None 1 3 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358545 235161 0 None 1 3 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722941 235165 0 None 1 3 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358549 235165 0 None 1 3 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722933 235158 0 None 1 3 Mouse 10.3 pEC50 = 10.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358541 235158 0 None 1 3 Mouse 10.3 pEC50 = 10.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
1324 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
16197727 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
4836 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
CHEMBL3629347 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
CHEMBL441738 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
DB04931 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0492756
122194229 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
1324 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
16197727 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
4836 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
CHEMBL3629347 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
CHEMBL441738 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
DB04931 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
118722944 235168 0 None -1 3 Mouse 10.2 pEC50 = 10.2 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358552 235168 0 None -1 3 Mouse 10.2 pEC50 = 10.2 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
1324 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
16197727 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
4836 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
CHEMBL3629347 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
CHEMBL441738 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
DB04931 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010524p
122194229 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
1324 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
16197727 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
4836 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
CHEMBL3629347 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
CHEMBL441738 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
DB04931 621 23 None -4 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303608
CHEMBL414965 488377 0 None -1 5 Mouse 10.1 pEC50 = 10.1 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1117 18 15 13 -2.5 C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
122194229 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
1324 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
16197727 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
4836 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
CHEMBL3629347 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
CHEMBL441738 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
DB04931 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm701093y
122194229 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
1324 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
16197727 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
4836 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
CHEMBL3629347 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
CHEMBL441738 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
DB04931 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0490843
122194229 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
1324 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
16197727 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
4836 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
CHEMBL3629347 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
CHEMBL441738 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
DB04931 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.0c00561
118722930 235156 0 None 1 3 Mouse 10.1 pEC50 = 10.1 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358539 235156 0 None 1 3 Mouse 10.1 pEC50 = 10.1 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
1324 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
16197727 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
4836 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
CHEMBL3629347 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
CHEMBL441738 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
DB04931 621 23 None -4 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm010061n
CHEMBL405087 487843 0 None -1 5 Mouse 10.0 pEC50 = 10 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1095 18 14 14 -1.8 C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
122194229 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
1324 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
16197727 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
4836 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
CHEMBL3629347 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
CHEMBL441738 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
DB04931 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00641
122194229 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
1324 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
16197727 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
4836 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
CHEMBL3629347 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
CHEMBL441738 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
DB04931 621 23 None -4 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.6b01707
CHEMBL406842 487926 0 None 3 5 Mouse 10.0 pEC50 = 10.0 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1129 18 14 14 -1.1 C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL413212 488271 0 None -6 4 Mouse 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 1058 17 13 11 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
127036484 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
1323 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
92432 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
CHEMBL430239 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
CHEMBL410404 488116 0 None 11 5 Mouse 9.9 pEC50 = 9.9 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1095 18 14 14 -1.8 C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
118722926 235153 0 None -1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358535 235153 0 None -1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
118722931 235157 0 None 1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358540 235157 0 None 1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
118722938 235162 0 None -1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358546 235162 0 None -1 3 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
1324 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
16197727 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
4836 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
CHEMBL3629347 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
CHEMBL441738 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
DB04931 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
127036484 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
1323 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
92432 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
CHEMBL430239 5482 39 None -4 7 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2015.10.095
122194229 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
1324 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
16197727 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
4836 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
CHEMBL3629347 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
CHEMBL441738 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
DB04931 621 23 None -4 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00684
CHEMBL411400 488173 0 None 48 5 Mouse 9.9 pEC50 = 9.9 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1123 18 14 14 -1.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O 10.1021/jm030452x
118722942 235166 0 None -1 3 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358550 235166 0 None -1 3 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722943 235167 0 None -1 3 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358551 235167 0 None -1 3 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
127036484 5482 39 None -4 7 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm010524p
1323 5482 39 None -4 7 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm010524p
92432 5482 39 None -4 7 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm010524p
CHEMBL3735690 5482 39 None -4 7 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm010524p
CHEMBL430239 5482 39 None -4 7 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm010524p
44310104 163022 0 None -7 3 Mouse 9.8 pEC50 = 9.8 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
CHEMBL216295 163022 0 None -7 3 Mouse 9.8 pEC50 = 9.8 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
CHEMBL2371851 477423 0 None -3 3 Mouse 9.8 pEC50 = 9.8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1025 21 12 12 -0.6 CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0490843
CHEMBL405335 487858 0 None 2 3 Mouse 9.8 pEC50 = 9.8 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1067 30 13 12 -1.7 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
118722927 235154 0 None 1 3 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358536 235154 0 None 1 3 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
1324 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
16197727 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
4836 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
CHEMBL3629347 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
CHEMBL441738 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
DB04931 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.10.095
122194229 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
1324 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
16197727 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
4836 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
CHEMBL3629347 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
CHEMBL441738 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
DB04931 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00301
127036484 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0492756
1323 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0492756
92432 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0492756
CHEMBL3735690 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0492756
CHEMBL430239 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0492756
122194229 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
1324 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
16197727 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
4836 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
CHEMBL3629347 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
CHEMBL441738 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
DB04931 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00856
127036484 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm501027w
1323 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm501027w
92432 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm501027w
CHEMBL3735690 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm501027w
CHEMBL430239 5482 39 None -4 7 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
1324 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
16197727 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
4836 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
CHEMBL3629347 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
CHEMBL441738 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
DB04931 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.3c00432
122194229 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
1324 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
16197727 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
4836 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
CHEMBL3629347 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
CHEMBL441738 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
DB04931 621 23 None -4 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.1c01417
CHEMBL214332 485136 29 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
CHEMBL214332 485136 29 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
CHEMBL408843 488035 0 None None None Human 9.7 pEC50 = 9.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 1125 15 14 14 -1.6 CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
118722932 234456 0 None 1 3 Mouse 9.6 pEC50 = 9.6 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3352878 234456 0 None 1 3 Mouse 9.6 pEC50 = 9.6 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL2371969 485798 0 None 1445 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1017 13 9 9 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0614275
122194229 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
1324 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
16197727 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
4836 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL3629347 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL441738 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
DB04931 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
122194229 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
1324 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
16197727 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
4836 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
CHEMBL3629347 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
CHEMBL441738 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
DB04931 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm800291b
122194229 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
1324 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
16197727 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
4836 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
CHEMBL3629347 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
CHEMBL441738 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
DB04931 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm500064t
122194229 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
1324 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
16197727 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
4836 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
CHEMBL3629347 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
CHEMBL441738 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
DB04931 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/j.bmcl.2015.09.046
122194229 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
1324 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
16197727 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
4836 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
CHEMBL3629347 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
CHEMBL441738 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
DB04931 621 23 None -4 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm301253y
CHEMBL2371971 485800 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1051 13 9 9 3.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O 10.1021/jm0614275
CHEMBL501592 488985 0 None 426 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1091 16 15 11 -0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
134463477 315101 0 None 3 3 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4099127 315101 0 None 3 3 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
122194229 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
1324 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
16197727 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
4836 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
CHEMBL3629347 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
CHEMBL441738 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
DB04931 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acsmedchemlett.9b00198
122194229 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
1324 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
16197727 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
4836 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
CHEMBL3629347 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
CHEMBL441738 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
DB04931 621 23 None -4 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.5b01894
45487403 394521 0 None -33 4 Mouse 9.5 pEC50 = 9.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569693 394521 0 None -33 4 Mouse 9.5 pEC50 = 9.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
118722936 235160 0 None -3 3 Mouse 9.5 pEC50 = 9.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358544 235160 0 None -3 3 Mouse 9.5 pEC50 = 9.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL2371962 485793 0 None 8 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1055 14 10 10 2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
CHEMBL267794 486241 0 None -11 3 Mouse 9.4 pEC50 = 9.4 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 927 28 12 10 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
122194229 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
1324 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
16197727 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
4836 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL3629347 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL441738 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
DB04931 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL214332 485136 29 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2003.08.078
122194229 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
1324 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
16197727 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
4836 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL3629347 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL441738 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
DB04931 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL214332 485136 29 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
CHEMBL307457 486457 0 None 10 3 Mouse 9.4 pEC50 = 9.4 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 814 23 11 9 -1.2 CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL266417 484238 0 None -12 5 Mouse 9.4 pEC50 = 9.4 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL214332 485136 29 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010524p
CHEMBL214332 485136 29 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303608
CHEMBL2371967 485797 0 None 288 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1077 12 8 9 3.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
134466953 312576 0 None -1 3 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4069451 312576 0 None -1 3 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
122194229 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
1324 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
16197727 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
4836 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
CHEMBL3629347 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
CHEMBL441738 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
DB04931 621 23 None -4 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.4c01556
90643803 221233 0 None 1 4 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 221233 0 None 1 4 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL386081 487686 0 None -25 3 Mouse 9.3 pEC50 = 9.3 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1450 46 21 19 -4.4 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010061n
CHEMBL429236 488542 0 None -21 3 Mouse 9.3 pEC50 = 9.3 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1309 40 16 15 -1.7 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
10864861 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
10886436 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
10952071 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
1338 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
9938402 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
CHEMBL140108 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
CHEMBL334457 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
CHEMBL339053 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
CHEMBL342954 8293 40 None 5 9 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02041
CHEMBL214332 485136 29 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL410763 488135 0 None -14 3 Mouse 9.3 pEC50 = 9.3 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 1265 38 18 16 -3.2 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL2369484 477577 0 None -3 3 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1528 24 22 21 -4.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL411378 488171 0 None 16 5 Mouse 9.3 pEC50 = 9.3 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1109 18 14 14 -1.5 Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1 10.1021/jm030452x
44310344 197639 0 None -3 3 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
77231883 197639 0 None -3 3 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL269274 197639 0 None -3 3 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
10078903 140291 0 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191303 140291 0 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
122194229 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
1324 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
16197727 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
4836 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL3629347 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL441738 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
DB04931 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
122194229 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
1324 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
16197727 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
4836 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL3629347 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL441738 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
DB04931 621 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL214332 485136 29 None -2 8 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
CHEMBL264536 486139 12 None -13 3 Mouse 9.2 pEC50 = 9.2 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 984 30 13 11 -1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm010061n
90643806 221236 0 None 6 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 221236 0 None 6 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL428801 488525 0 None -12 5 Mouse 9.2 pEC50 = 9.2 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 1149 17 13 11 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
101670969 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
16131138 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
44349184 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
53310908 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
91898438 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL438402 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
DB15687 333535 25 None -1 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL214332 485136 29 None -2 8 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
122184910 241128 0 None 28 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 241128 0 None 28 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL214332 485136 29 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
90643802 221232 0 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 221232 0 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
11158573 143350 0 None -2 3 Mouse 9.1 pEC50 = 9.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL195439 143350 0 None -2 3 Mouse 9.1 pEC50 = 9.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
137637283 311907 0 None -2 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 311907 0 None -2 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL2371968 477721 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1069 12 8 9 4.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL2371970 485799 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1057 13 9 9 3.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C2CCCCC2)NC1=O 10.1021/jm0614275
90643808 221237 0 None 7 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 221237 0 None 7 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
122194229 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
1324 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
16197727 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
4836 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL3629347 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL441738 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
DB04931 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
122194229 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
1324 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
16197727 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
4836 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL3629347 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL441738 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
DB04931 621 23 None -9 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
122194229 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
1324 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
16197727 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
4836 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
CHEMBL3629347 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
CHEMBL441738 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
DB04931 621 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
122184635 241007 0 None 10 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None 10 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
90643804 221234 0 None 2 4 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 221234 0 None 2 4 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL214332 485136 29 None -2 8 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
CHEMBL2096742 484199 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm801300c
CHEMBL428615 488519 0 None -70 5 Mouse 8.9 pEC50 = 8.9 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 1042 17 13 11 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
155553683 348243 0 None -8 3 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155564058 348243 0 None -8 3 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4547556 348243 0 None -8 3 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4574056 348243 0 None -8 3 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL1688107 484745 0 None -8 3 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1506 23 20 19 -1.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL491870 488927 0 None -3 4 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 719 18 10 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
127036484 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
1323 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
92432 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
CHEMBL3735690 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
CHEMBL430239 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
CHEMBL2371963 485794 0 None 218 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1001 12 8 9 2.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL500743 488968 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1041 16 15 11 -2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL322610 486642 0 None 2 4 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 811 18 10 7 0.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
155550083 347987 0 None 5 3 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155555217 347987 0 None 5 3 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4540411 347987 0 None 5 3 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550976 347987 0 None 5 3 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
127036484 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
1323 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
92432 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL3735690 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL430239 5482 39 None -151 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
118722939 235163 0 None -3 3 Mouse 8.8 pEC50 = 8.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358547 235163 0 None -3 3 Mouse 8.8 pEC50 = 8.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL2370966 485649 0 None None None Human 8.7 pEC50 = 8.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1525 47 20 18 -3.0 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
118722940 235164 0 None -2 3 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358548 235164 0 None -2 3 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358537 486963 0 None -7 3 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 33 13 11 0.8 C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
145976863 328725 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 328725 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL503229 489006 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1593 48 23 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL443071 488858 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1609 48 21 20 -2.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
118722935 235159 0 None -1 3 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358543 235159 0 None -1 3 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
122194229 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
1324 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
16197727 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
4836 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
CHEMBL3629347 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
CHEMBL441738 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
DB04931 621 23 None -4 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00053
11787684 142519 0 None -3 3 Mouse 8.0 pEC50 = 8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL194217 142519 0 None -3 3 Mouse 8.0 pEC50 = 8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3752534 487533 1 None -5 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1131 15 12 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
10483153 123575 0 None -56 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 123575 0 None -56 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
49862377 38939 0 None -91 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 38939 0 None -91 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
132180599 312503 0 None -2 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
137632948 312503 0 None -2 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4068643 312503 0 None -2 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4072129 312503 0 None -2 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
44401319 26552 0 None -10 2 Human 6.0 pEC50 = 6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1184826 26552 0 None -10 2 Human 6.0 pEC50 = 6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL407213 487949 0 None None None Human 6.0 pEC50 = 6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 823 10 10 8 -0.2 CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
178322595 467156 0 None -1 3 Human 5.0 pEC50 = 5 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 453 8 2 5 4.6 CCc1ccc(-c2cc(CNC3CCN(c4ccccc4C(N)=O)C3)c(OC)cc2F)s1 10.1021/acs.jmedchem.4c01763
CHEMBL6170004 467156 0 None -1 3 Human 5.0 pEC50 = 5 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 453 8 2 5 4.6 CCc1ccc(-c2cc(CNC3CCN(c4ccccc4C(N)=O)C3)c(OC)cc2F)s1 10.1021/acs.jmedchem.4c01763
155555947 348560 0 None -77 2 Mouse 5.0 pEC50 = 5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4555150 348560 0 None -77 2 Mouse 5.0 pEC50 = 5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
11017471 65544 0 None -104 2 Human 6.0 pEC50 = 6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1 10.1021/jm025539h
CHEMBL140738 65544 0 None -104 2 Human 6.0 pEC50 = 6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1 10.1021/jm025539h
44448629 327664 0 None -204 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 327664 0 None -204 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
178312562 466853 0 None -1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 788 23 7 8 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6162652 466853 0 None -1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 788 23 7 8 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL50056 484368 1 None -8 6 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL50056 484368 1 None -8 6 Mouse 7.0 pEC50 = 7.0 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
164621851 369144 0 None None None Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 13 3 3 5.8 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4867949 369144 0 None None None Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 13 3 3 5.8 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
45487296 394414 0 None -8 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568836 394414 0 None -8 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
45487416 394115 0 None -9 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567039 394115 0 None -9 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL3600833 487196 0 None -20 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
137633806 312402 0 None -38 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 312402 0 None -38 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL264190 484234 0 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
155563055 349305 0 None -2 3 Mouse 8.0 pEC50 = 8.0 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4573041 349305 0 None -2 3 Mouse 8.0 pEC50 = 8.0 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL319871 486633 0 None 2 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 761 19 9 7 1.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL2323791 477559 0 None 4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1585 21 19 21 -2.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44441637 194464 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 506 7 2 4 4.3 CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248892 194464 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 506 7 2 4 4.3 CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44441685 194545 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249322 194545 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL319922 486634 0 None 1 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 735 18 9 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL2448525 486015 0 None -177 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL102391 484393 0 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 699 19 9 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
45487404 394522 0 None -2344 4 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569694 394522 0 None -2344 4 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44408388 277611 0 None -79 3 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 277611 0 None -79 3 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
155547842 347780 0 None -50 3 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4535510 347780 0 None -50 3 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44448479 308745 0 None -10 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 308745 0 None -10 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
44310242 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44310243 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932909 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932912 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL406550 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL440633 312232 0 None 3 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL2323529 477552 0 None -1 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1520 21 19 21 -3.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
178313279 466750 0 None -2 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 786 22 8 6 3.5 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6160142 466750 0 None -2 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 786 22 8 6 3.5 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
168285801 374542 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 374542 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
164623712 368945 0 None None None Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 13 3 3 5.3 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4864765 368945 0 None None None Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 13 3 3 5.3 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
11061068 64921 0 None -120 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
44441641 64921 0 None -120 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 64921 0 None -120 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL250508 64921 0 None -120 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
45487407 394069 0 None -7 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566545 394069 0 None -7 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
155556047 348545 0 None 2 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155566298 348545 0 None 2 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4554828 348545 0 None 2 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4584189 348545 0 None 2 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155561743 349571 0 None -1 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155565321 349571 0 None -1 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4579448 349571 0 None -1 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4583714 349571 0 None -1 3 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
164624151 369083 0 None None None Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866885 369083 0 None None None Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164626157 369661 0 None None None Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4875776 369661 0 None None None Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
137653704 314500 0 None -3 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4092424 314500 0 None -3 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155550338 348364 0 None -18 2 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 649 17 10 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550246 348364 0 None -18 2 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 649 17 10 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
178300807 466192 0 None 2 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 480 9 1 5 4.7 COc1ccc(C(CN(C)C)NC(=O)COc2ccc(-c3cccc4c3OCC4)cc2Cl)cc1 10.1021/acs.jmedchem.4c01763
CHEMBL6132827 466192 0 None 2 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 480 9 1 5 4.7 COc1ccc(C(CN(C)C)NC(=O)COc2ccc(-c3cccc4c3OCC4)cc2Cl)cc1 10.1021/acs.jmedchem.4c01763
CHEMBL2369131 485401 0 None -3 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
178322982 466978 0 None -3 3 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 814 23 8 7 2.6 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6165640 466978 0 None -3 3 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 814 23 8 7 2.6 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
137638778 312675 0 None -81 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 312675 0 None -81 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
178307969 467171 0 None -2 3 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 723 20 6 6 3.7 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](C(C)C)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6170426 467171 0 None -2 3 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 723 20 6 6 3.7 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](C(C)C)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
145966490 329307 0 None -2 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 329307 0 None -2 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145975465 328911 0 None -20 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 328911 0 None -20 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
164623811 369182 0 None 1 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868636 369182 0 None 1 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
155538472 347353 0 None -3 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155548791 347353 0 None -3 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4524668 347353 0 None -3 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4536340 347353 0 None -3 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL427629 488478 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
54584302 123576 0 None -24 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 123576 0 None -24 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
44401315 26551 0 None -33 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1184825 26551 0 None -33 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
90661465 155051 0 None -38 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2078649 155051 0 None -38 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2304247 485327 0 None -213 3 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL589515 489304 0 None -2 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 653 17 9 6 0.7 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmc.2009.12.010
178318772 466486 0 None 1 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 699 19 6 6 2.9 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCO)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2C)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6146793 466486 0 None 1 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 699 19 6 6 2.9 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCO)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2C)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
46885368 22272 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
CHEMBL1090484 22272 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
44305885 468135 0 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 474 13 4 4 3.5 NCCCCNC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL63867 468135 0 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 474 13 4 4 3.5 NCCCCNC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
122184911 241129 0 None -25 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 241129 0 None -25 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL214332 485136 29 None -2 8 Mouse 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
164610489 367864 0 None 1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 10 4 4 5.8 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4848322 367864 0 None 1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 10 4 4 5.8 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL228194 485299 0 None -30 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 995 13 10 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
46885863 22786 0 None -41 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1093858 22786 0 None -41 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL3601431 487209 0 None -3 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
178310238 467421 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 725 21 7 7 2.4 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6175807 467421 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 725 21 7 7 2.4 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
122184575 241001 0 None -42 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 241001 0 None -42 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
51350911 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351024 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318435 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322399 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932357 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932358 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688106 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688109 121588 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL602651 489321 0 None -1 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 809 22 10 8 -0.6 CC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1 10.1016/j.bmc.2009.12.010
162661397 355373 0 None 2 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162671821 355373 0 None 2 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4765156 355373 0 None 2 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4792291 355373 0 None 2 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
137648053 313436 0 None 3 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4080169 313436 0 None 3 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL343094 487089 0 None 1 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 18 8 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
16725559 195368 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 195368 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
164613912 368070 0 None 6 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 12 3 3 4.9 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4851040 368070 0 None 6 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 12 3 3 4.9 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
137640475 312998 0 None -36 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4074368 312998 0 None -36 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
178297566 466670 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 400 5 1 3 4.8 Cc1ccc(-c2cc(Cl)cs2)cc1C1(C(=O)NC2CN(C3CCC3)C2)CC1 10.1021/acs.jmedchem.4c01763
CHEMBL6151620 466670 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 400 5 1 3 4.8 Cc1ccc(-c2cc(Cl)cs2)cc1C1(C(=O)NC2CN(C3CCC3)C2)CC1 10.1021/acs.jmedchem.4c01763
171378343 388754 0 None -14 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5423711 388754 0 None -14 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
46232220 451506 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602652 451506 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487295 394461 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569221 394461 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44448590 195963 0 None -36 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 195963 0 None -36 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL432895 488586 3 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 548 14 7 5 -0.0 CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL3601426 487208 0 None -2089 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600832 487195 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371965 477720 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1055 12 8 9 3.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
132180597 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
132180653 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4063911 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4567961 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL214332 485136 29 None -64 8 Human 7.8 pEC50 = 7.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
CHEMBL214332 485136 29 None -64 8 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
CHEMBL214332 485136 29 None -64 8 Human 7.8 pEC50 = 7.8 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL451423 488895 0 None -1 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 730 19 10 9 -0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
145964017 328999 0 None -52 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 328999 0 None -52 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
122194229 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
1324 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
16197727 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
4836 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
CHEMBL3629347 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
CHEMBL441738 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
DB04931 621 23 None -4 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00318-4
10146211 136659 0 None -288 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 136659 0 None -288 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
44323234 40519 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347221 40519 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 40519 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432377 40519 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
9852256 349371 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4574756 349371 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
164609931 367806 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 12 3 3 5.6 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4847357 367806 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 12 3 3 5.6 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
44457021 198200 0 None -9 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL272439 198200 0 None -9 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
44441646 310159 0 None -16 3 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 310159 0 None -16 3 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487288 394445 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569076 394445 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
46885815 22177 0 None -389 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
CHEMBL1089830 22177 0 None -389 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
145964837 329293 0 None -2 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 329293 0 None -2 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
137656489 315544 0 None 1 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4104402 315544 0 None 1 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
162666503 356057 0 None -15 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
162670795 356057 0 None -15 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4783292 356057 0 None -15 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4791112 356057 0 None -15 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
132180597 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
132180653 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4063911 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567961 312095 0 None -20 2 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155558348 349063 0 None 5 3 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567480 349063 0 None 5 3 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL420167 488424 0 None None None Human 7.8 pEC50 = 7.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 918 11 12 10 -0.9 NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL427205 488473 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 829 13 10 8 0.0 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
164624627 369162 0 None 2 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868223 369162 0 None 2 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
44431512 292638 0 None 5 3 Human 6.8 pEC50 = 6.8 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 292638 0 None 5 3 Human 6.8 pEC50 = 6.8 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
46885759 22592 0 None -295 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092548 22592 0 None -295 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
164628926 369779 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 14 3 3 6.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4877537 369779 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 14 3 3 6.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL3349030 486807 0 None -14 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
71449119 160461 0 None -138 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL2113028 160461 0 None -138 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
155538874 346918 0 None 1 2 Mouse 5.8 pEC50 = 5.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4513460 346918 0 None 1 2 Mouse 5.8 pEC50 = 5.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137649203 313406 0 None -10 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079721 313406 0 None -10 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
45487289 394450 0 None -10 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 590 17 8 7 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccnc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569104 394450 0 None -10 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 590 17 8 7 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccnc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2304250 485329 0 None -2 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL431242 488575 0 None 1 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 724 18 10 7 -0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
45487408 393942 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
45487417 393942 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL565927 393942 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL567233 393942 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
164616640 367874 0 None None None Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 13 3 3 6.0 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4848447 367874 0 None None None Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 13 3 3 6.0 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL268851 486276 0 None None None Human 7.7 pEC50 = 7.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44348144 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None -66 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44401323 26075 0 None -46 2 Human 5.7 pEC50 = 5.7 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 569 7 4 5 3.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1181891 26075 0 None -46 2 Human 5.7 pEC50 = 5.7 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 569 7 4 5 3.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
44391999 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None -120 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
45487291 394460 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569220 394460 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
11328898 22276 25 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 22276 25 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
DB12517 22276 25 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44441687 194420 0 None -34 2 Human 5.7 pEC50 = 5.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.3 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL248671 194420 0 None -34 2 Human 5.7 pEC50 = 5.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.3 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
44396986 139715 0 None -28 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 139715 0 None -28 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 139715 0 None -28 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 139715 0 None -28 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2304246 485326 0 None -3 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
145971389 329563 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 329563 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
15603023 198263 0 None 1 3 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL272660 198263 0 None 1 3 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL214332 485136 29 None -2 8 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
CHEMBL444219 488866 0 None -4 3 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 703 18 10 7 -0.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
127046235 276946 0 None 2 4 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3797690 276946 0 None 2 4 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
137656180 314883 0 None 5 3 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4096678 314883 0 None 5 3 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
132180598 313735 0 None -7 3 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155543031 313735 0 None -7 3 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4083717 313735 0 None -7 3 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4522298 313735 0 None -7 3 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL406891 487928 0 None 2 5 Mouse 8.7 pEC50 = 8.7 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1109 18 14 14 -1.4 C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL1688107 484745 0 None -8 3 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1506 23 20 19 -1.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
127035019 7320 11 None -2 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.5b00184
1325 7320 11 None -2 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.5b00184
9898183 7320 11 None -2 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.5b00184
CHEMBL3422426 7320 11 None -2 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.5b00184
CHEMBL3735607 7320 11 None -2 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.5b00184
CHEMBL3287327 486718 0 None 1 4 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
44400428 253674 0 None -2 3 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL364726 253674 0 None -2 3 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44422999 333494 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 333494 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL502093 488993 0 None -2 3 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 763 18 10 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
122194229 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
1324 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
16197727 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
4836 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
CHEMBL3629347 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
CHEMBL441738 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
DB04931 621 23 None -4 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.0c02041
CHEMBL370254 487483 3 None 6 3 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 643 17 9 7 -0.8 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm0490843
11263053 140292 0 None -3 3 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191304 140292 0 None -3 3 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL448536 488887 0 None -1 3 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 710 18 10 8 -0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
11423083 197165 0 None -3 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL265236 197165 0 None -3 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
101043845 332258 1 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
145948876 332258 1 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 332258 1 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5177536 332258 1 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
44456964 312608 0 None -1 3 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL406985 312608 0 None -1 3 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL204864 485037 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 893 15 10 8 1.7 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
137651071 313367 0 None -25 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079298 313367 0 None -25 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL438920 488753 0 None -99 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1578 47 20 20 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL433645 488592 0 None None None Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 781 9 10 8 -0.4 NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL409636 488073 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1604 35 21 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
CHEMBL375947 487549 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 964 13 10 10 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155512534 334261 0 None -22 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4437801 334261 0 None -22 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL320157 486635 0 None 1 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 645 15 7 6 -0.0 CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44391940 26520 0 None -7 2 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1184624 26520 0 None -7 2 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
46203215 22784 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 428 3 1 3 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1093856 22784 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 428 3 1 3 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44305712 202870 0 None -1 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 421 11 5 3 2.8 NCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305391 202870 0 None -1 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 421 11 5 3 2.8 NCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44359732 62733 0 None -2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 720 19 3 6 2.6 CC(=O)N(CC(=O)N(CC(=O)N(CCCCN=C(N)N)CC(=O)N(CC(N)=O)Cc1cccc2ccccc12)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL138100 62733 0 None -2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 720 19 3 6 2.6 CC(=O)N(CC(=O)N(CC(=O)N(CCCCN=C(N)N)CC(=O)N(CC(N)=O)Cc1cccc2ccccc12)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
164616687 367933 0 None 11 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 13 3 3 5.0 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4849344 367933 0 None 11 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 13 3 3 5.0 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL2323793 477561 0 None -27 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1685 23 20 21 -0.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44335147 18936 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 18936 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL524861 489128 0 None 1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1041 16 15 11 -2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
54587278 123582 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 123582 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
137639815 312719 0 None -3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4071063 312719 0 None -3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
6918780 126174 0 None -478 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
CHEMBL179836 126174 0 None -478 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
44347220 333129 0 None None None Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 333129 0 None None None Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL2370965 485648 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1586 47 19 17 -0.7 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL607104 489332 0 None 2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 697 15 8 7 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
164621664 368856 0 None None None Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 14 3 3 5.4 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4863313 368856 0 None None None Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 14 3 3 5.4 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL454736 488907 0 None 4 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 735 18 10 7 0.8 CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL50056 484368 1 None -8 6 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44347331 40216 0 None None None Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None None None Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
11061068 64921 0 None -120 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44441641 64921 0 None -120 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL140154 64921 0 None -120 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 64921 0 None -120 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL3350327 486866 0 None -13 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
44310258 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44310259 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932908 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932914 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL410091 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL413465 315262 0 None 4 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL500516 488963 0 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 700 18 11 8 -0.8 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
45487413 394340 0 None -1 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568409 394340 0 None -1 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
44445083 310362 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 310362 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
164609002 367698 0 None None None Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164622957 367698 0 None None None Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4845749 367698 0 None None None Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4871777 367698 0 None None None Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
9808720 136553 0 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
9960253 136553 0 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL180892 136553 0 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL338594 136553 0 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
45487287 404432 0 None -3 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL570903 404432 0 None -3 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
46232224 451509 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602654 451509 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487300 394448 0 None -7 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569086 394448 0 None -7 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
122184637 241009 0 None -10 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 241009 0 None -10 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
155561743 349571 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155565321 349571 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4579448 349571 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4583714 349571 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44347331 40216 0 None None None Human 6.6 pEC50 = 6.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None None None Human 6.6 pEC50 = 6.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL509582 489086 0 None -12 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1072 14 13 11 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44401585 28012 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1195347 28012 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
15953833 160466 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 5 receptor in cAMP release assayEffective concentration against human melanocortin 5 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 160466 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 5 receptor in cAMP release assayEffective concentration against human melanocortin 5 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
155538472 347353 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155548791 347353 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4524668 347353 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4536340 347353 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162666503 356057 0 None -15 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
162670795 356057 0 None -15 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4783292 356057 0 None -15 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4791112 356057 0 None -15 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
127036484 5482 39 None -151 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
1323 5482 39 None -151 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
92432 5482 39 None -151 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
CHEMBL3735690 5482 39 None -151 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
CHEMBL430239 5482 39 None -151 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
137649368 313306 0 None -53 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
137657607 313306 0 None -53 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4078495 313306 0 None -53 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103567 313306 0 None -53 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
44441644 310857 0 None -64 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 310857 0 None -64 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL2310901 485337 0 None -19 4 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1523 44 18 17 -1.2 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL455070 488908 0 None -58 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1022 14 13 11 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
178315669 467410 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 820 24 9 7 2.7 N=C(N)NCCC[C@H]1CN(CCN(CCN2C[C@H](Cc3c[nH]cn3)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
CHEMBL6175484 467410 0 None -3 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 820 24 9 7 2.7 N=C(N)NCCC[C@H]1CN(CCN(CCN2C[C@H](Cc3c[nH]cn3)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
44457067 198045 0 None -5 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL271586 198045 0 None -5 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
162654633 354516 0 None -18 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162672755 354516 0 None -18 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4754987 354516 0 None -18 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 354516 0 None -18 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
137636060 312155 0 None None None Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4064728 312155 0 None None None Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
44335147 18936 0 None 4 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 18936 0 None 4 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
178314694 467225 0 None None None Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 722 20 6 7 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6171577 467225 0 None None None Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 722 20 6 7 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL3350396 486875 0 None -891 4 Human 6.6 pEC50 = 6.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1095 17 14 12 -1.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL376614 487569 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1009 14 10 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL2323790 477558 0 None -8 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1595 21 18 20 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137653916 314450 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4091894 314450 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155567887 350021 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4590532 350021 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL263878 486112 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL3349030 486807 0 None -14 3 Human 5.6 pEC50 = 5.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44391999 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
10864861 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
10886436 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
10952071 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
1338 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL140108 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL334457 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL342954 8293 40 None -1659 9 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
155545201 347544 0 None -1 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 602 14 6 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4529287 347544 0 None -1 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 602 14 6 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
10864861 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -1659 9 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
45487411 394140 0 None -10 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567240 394140 0 None -10 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL266417 484238 0 None -776 5 Human 7.6 pEC50 = 7.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL2370963 485646 0 None 85 2 Human 7.6 pEC50 = 7.6 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1562 47 20 18 -2.4 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44408190 197247 0 None -48 3 Human 6.6 pEC50 = 6.6 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 197247 0 None -48 3 Human 6.6 pEC50 = 6.6 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
10257242 38928 0 None -79 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 38928 0 None -79 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL430843 488572 0 None 2 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 699 19 9 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
122178163 239864 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 998 10 10 10 0.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)c2cc3ccccc3cc2NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577992 239864 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 998 10 10 10 0.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)c2cc3ccccc3cc2NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
155554244 348979 0 None -15 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4565607 348979 0 None -15 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44305763 468133 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL63850 468133 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL2323786 477554 0 None -2 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 23 19 21 -1.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL214332 485136 29 None -64 8 Human 7.5 pEC50 = 7.5 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
137634306 312245 0 None -2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
137646614 312245 0 None -2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4065669 312245 0 None -2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4080138 312245 0 None -2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
172449425 388312 0 None -2187 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5414451 388312 0 None -2187 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
46232222 451508 0 None -4 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602653 451508 0 None -4 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
44441648 310723 0 None -18 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 310723 0 None -18 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137635422 311837 0 None -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
137636428 311837 0 None -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 311837 0 None -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4062443 311837 0 None -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL264190 484234 0 None -1 7 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
90643805 221235 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 221235 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155544214 347430 0 None 1 2 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 797 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4526652 347430 0 None 1 2 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 797 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155549760 347952 0 None -11 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155563222 347952 0 None -11 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539621 347952 0 None -11 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4572994 347952 0 None -11 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155550083 347987 0 None 5 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155555217 347987 0 None 5 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4540411 347987 0 None 5 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550976 347987 0 None 5 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
11308957 141646 0 None -1 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL193151 141646 0 None -1 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL264190 484234 0 None -1 7 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
127047475 277054 0 None 1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
132991507 277054 0 None 1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798421 277054 0 None 1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL439128 488768 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL3358533 486962 0 None -7 3 Mouse 8.5 pEC50 = 8.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 33 13 11 0.8 C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL264190 484234 0 None -1 7 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
127036484 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
1323 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
92432 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL3735690 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL430239 5482 39 None -151 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL393075 487766 0 None -10 4 Human 8.5 pEC50 = 8.5 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1032 16 14 11 -0.1 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
11239907 260988 0 None -5 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL370261 260988 0 None -5 3 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
155553683 348243 0 None -8 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155564058 348243 0 None -8 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4547556 348243 0 None -8 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4574056 348243 0 None -8 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL264190 484234 0 None -1 7 Mouse 8.5 pEC50 = 8.5 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
162649653 353982 0 None -12 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162673830 353982 0 None -12 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4748317 353982 0 None -12 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4795352 353982 0 None -12 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL2370964 485647 0 None -8 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL4299619 477445 0 None 1 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 2236 54 25 25 -5.6 CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL2370964 485647 0 None -8 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL264190 484234 0 None 1 7 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL264190 484234 0 None 1 7 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.2c01794
127047913 277224 0 None 4 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799563 277224 0 None 4 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL264190 484234 0 None -1 7 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
164612516 368684 0 None None None Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860714 368684 0 None None None Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL510687 489095 0 None -3 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 719 18 10 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
155556047 348545 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155566298 348545 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4554828 348545 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4584189 348545 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL203602 485031 0 None 3 3 Human 6.5 pEC50 = 6.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 858 15 11 9 -1.4 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
155531140 336150 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4465466 336150 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44401530 27060 0 None -42 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1188092 27060 0 None -42 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
44347119 233438 0 None None None Human 6.5 pEC50 = 6.5 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 233438 0 None None None Human 6.5 pEC50 = 6.5 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
45487405 394523 0 None -25 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 587 16 8 6 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569695 394523 0 None -25 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 587 16 8 6 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
51350673 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51350799 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53317148 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53323763 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932356 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932362 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688104 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688105 121587 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
44305704 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44305790 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305559 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL64954 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
45487294 393904 0 None -3 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565688 393904 0 None -3 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2371973 477723 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1083 13 8 9 3.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
162662213 355345 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162664463 355345 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4764827 355345 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4782762 355345 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162661724 355382 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
162665266 355382 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4765199 355382 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4782693 355382 0 None 3 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
46232223 429121 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589468 429121 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
178298635 466221 0 None 1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 454 6 2 5 5.0 O=C1NCCOc2ccc(CNCC3(c4ccc(C=C5CCSCC5)s4)CCC3)cc21 10.1021/acs.jmedchem.4c01763
CHEMBL6133378 466221 0 None 1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 454 6 2 5 5.0 O=C1NCCOc2ccc(CNCC3(c4ccc(C=C5CCSCC5)s4)CCC3)cc21 10.1021/acs.jmedchem.4c01763
178317350 466883 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 735 20 6 6 3.4 C[C@H]1CNC(=N)N1CCN(CCN1C[C@H](CCO)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
CHEMBL6163238 466883 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 735 20 6 6 3.4 C[C@H]1CNC(=N)N1CCN(CCN1C[C@H](CCO)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
CHEMBL302703 484250 0 None 4 4 Mouse 6.5 pEC50 = 6.5 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
46232228 451184 0 None 3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602299 451184 0 None 3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
44456958 197710 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
CHEMBL269837 197710 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
CHEMBL104880 484403 0 None 1 2 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 701 18 10 8 -0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44305704 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44305790 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305559 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL64954 202896 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44275650 194469 0 None -83 4 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 194469 0 None -83 4 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
127036484 5482 39 None -151 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
1323 5482 39 None -151 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
92432 5482 39 None -151 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
CHEMBL3735690 5482 39 None -151 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
CHEMBL430239 5482 39 None -151 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
137645483 313514 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 906 11 11 10 -1.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4081092 313514 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 906 11 11 10 -1.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
44391927 28233 0 None -114 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 28233 0 None -114 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
53318436 121589 0 None -2 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
CHEMBL1688108 121589 0 None -2 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
CHEMBL103817 484397 0 None -4 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 735 18 9 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44408286 277945 0 None -141 3 Human 6.5 pEC50 = 6.5 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 277945 0 None -141 3 Human 6.5 pEC50 = 6.5 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
137658359 315410 0 None -6 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102774 315410 0 None -6 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL488355 488925 0 None -3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 741 18 10 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(C)(C)C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164619151 368843 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4863206 368843 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
44401522 27049 0 None -112 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1188041 27049 0 None -112 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
44391938 26021 0 None -10 2 Human 6.5 pEC50 = 6.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1181567 26021 0 None -10 2 Human 6.5 pEC50 = 6.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
45487408 393942 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
45487417 393942 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL565927 393942 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL567233 393942 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
178313954 467264 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 763 21 6 6 4.1 CC(C)[C@H]1CN(CCN(CCN2C[C@H](Cc3c[nH]cn3)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
CHEMBL6172334 467264 0 None -6 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 763 21 6 6 4.1 CC(C)[C@H]1CN(CCN(CCN2C[C@H](Cc3c[nH]cn3)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
CHEMBL602650 489320 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 809 22 10 8 -0.6 CC(=O)NCC(=O)N(CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1 10.1016/j.bmc.2009.12.010
CHEMBL405282 487855 22 None -104 6 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/acs.jmedchem.5b01894
CHEMBL214332 485136 29 None -64 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL2323799 477567 0 None -22 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1649 24 20 21 -1.4 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
46232225 451697 0 None 4 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602852 451697 0 None 4 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
46885761 22344 0 None -56 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL1090813 22344 0 None -56 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL441988 488845 4 None 162 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 548 14 7 5 -0.0 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
162661724 355382 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
162665266 355382 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4765199 355382 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4782693 355382 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL389674 487742 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 964 13 10 10 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL214332 485136 29 None -64 8 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
CHEMBL138771 484676 0 None -1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 695 18 7 6 1.0 CC(=O)N(CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
44401528 28231 0 None -51 2 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1196956 28231 0 None -51 2 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
44408253 277631 0 None -257 4 Human 5.4 pEC50 = 5.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 277631 0 None -257 4 Human 5.4 pEC50 = 5.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
46885712 22387 0 None -204 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 22387 0 None -204 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL104052 484400 0 None -1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 686 18 9 8 -1.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
46885972 22435 0 None -52 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1091631 22435 0 None -52 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
145980719 331313 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 331313 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
172441600 387613 0 None -831 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@H](C(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL5399539 387613 0 None -831 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@H](C(N)=O)CS2 10.1021/acs.jmedchem.2c01587
44448660 195354 0 None -416 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 195354 0 None -416 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
137637656 312162 0 None -40 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 312162 0 None -40 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
164626210 369758 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 670 12 4 4 7.0 CC[C@H](C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccc(O)cc1)N1C[C@@H](Cc2ccccc2)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4877184 369758 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 670 12 4 4 7.0 CC[C@H](C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccc(O)cc1)N1C[C@@H](Cc2ccccc2)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44441643 310821 0 None -18 2 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400252 310821 0 None -18 2 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44347927 313181 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 313181 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
178323788 467380 0 None -2 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 784 23 9 7 2.1 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCCNC(=N)N)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6174972 467380 0 None -2 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 784 23 9 7 2.1 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCCNC(=N)N)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
162662213 355345 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162664463 355345 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4764827 355345 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4782762 355345 0 None 3 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
44457043 197915 0 None -2 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL270923 197915 0 None -2 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
178320756 467177 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 731 20 6 6 3.6 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6170574 467177 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 731 20 6 6 3.6 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
51350673 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51350799 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53317148 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53323763 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932356 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932362 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688104 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688105 121587 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL437050 484343 3 None -8 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44310242 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44310243 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932909 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932912 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL406550 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL440633 312232 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
178306286 467241 0 None -5 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 727 20 6 6 3.5 CC(C)[C@H]1CN(CCN(CCN2C[C@H]([C@@H](C)O)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
CHEMBL6171848 467241 0 None -5 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 727 20 6 6 3.5 CC(C)[C@H]1CN(CCN(CCN2C[C@H]([C@@H](C)O)N(CCc3ccc(F)cc3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCCC1CCCCC1 10.1021/acs.jmedchem.4c01556
46232221 429167 0 None -1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589516 429167 0 None -1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
178318965 466809 0 None -4 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 749 22 7 8 1.7 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6161576 466809 0 None -4 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 749 22 7 8 1.7 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
44305805 201024 0 None 1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 393 9 5 3 2.0 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL293673 201024 0 None 1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 393 9 5 3 2.0 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL264190 484234 0 None -1 7 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
127047853 277287 0 None 1 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799955 277287 0 None 1 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL264190 484234 0 None -1 7 Mouse 8.4 pEC50 = 8.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
155539948 347006 0 None -1 3 Mouse 8.4 pEC50 = 8.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4515666 347006 0 None -1 3 Mouse 8.4 pEC50 = 8.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL2370968 485651 0 None -3 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1561 44 19 17 -1.4 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370968 485651 0 None -3 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1561 44 19 17 -1.4 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL264190 484234 0 None -1 7 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.0c02041
CHEMBL385465 487662 0 None None None Human 8.4 pEC50 = 8.4 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 960 12 12 10 -0.8 CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL405791 487882 0 None 1 4 Mouse 8.4 pEC50 = 8.4 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1145 18 14 14 -0.7 C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ncc[nH]2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
11491374 139899 0 None -4 3 Mouse 8.4 pEC50 = 8.4 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL190366 139899 0 None -4 3 Mouse 8.4 pEC50 = 8.4 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
155567399 349941 0 None 17 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4588429 349941 0 None 17 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
11181928 331002 0 None -1 3 Mouse 8.3 pEC50 = 8.3 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL426282 331002 0 None -1 3 Mouse 8.3 pEC50 = 8.3 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3799094 487584 0 None 2 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1568 36 17 19 -6.0 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
137644449 314170 0 None 3 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4088980 314170 0 None 3 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
155542040 347191 0 None -131 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155568641 347191 0 None -131 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4519837 347191 0 None -131 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4591394 347191 0 None -131 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155549865 347932 0 None 10 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539175 347932 0 None 10 3 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
44408287 157053 0 None -309 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 157053 0 None -309 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44408275 157086 0 None -46 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 157086 0 None -46 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL3287060 486707 0 None -6 4 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 711 18 10 7 0.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL317228 486610 0 None 3 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 671 17 9 7 -0.5 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)c1ccccc1 10.1021/jm010524p
178300981 466340 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 432 7 1 3 5.0 CCCN1CC(NC(=O)[C@@H]2C[C@H]2c2cccc(-c3cc(Cl)ccc3OC)c2Cl)C1 10.1021/acs.jmedchem.4c01763
CHEMBL6143005 466340 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 432 7 1 3 5.0 CCCN1CC(NC(=O)[C@@H]2C[C@H]2c2cccc(-c3cc(Cl)ccc3OC)c2Cl)C1 10.1021/acs.jmedchem.4c01763
178296548 466735 0 None None None Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 429 7 3 6 3.7 CNc1cc(N2C[C@H](O)C[C@@H]2CNC2CC(c3cccc(-c4ccccc4)c3)C2)ncn1 10.1021/acs.jmedchem.4c01763
CHEMBL6159657 466735 0 None None None Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 429 7 3 6 3.7 CNc1cc(N2C[C@H](O)C[C@@H]2CNC2CC(c3cccc(-c4ccccc4)c3)C2)ncn1 10.1021/acs.jmedchem.4c01763
155558598 348798 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 656 13 5 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4561005 348798 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 656 13 5 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL2096759 485069 0 None -51 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
137640715 312913 0 None -56 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4073316 312913 0 None -56 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
118735100 237588 0 None -316 3 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 237588 0 None -316 3 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL104010 484399 0 None -1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 675 18 10 8 -1.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL2323789 477557 0 None -213 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1645 23 19 20 -0.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2370553 477661 0 None None None Human 7.4 pEC50 = 7.4 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 1520 26 17 20 -2.1 CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
155566074 349720 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582914 349720 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL106959 484409 0 None -2 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 761 19 9 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm010524p
145989222 332071 0 None -67 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 332071 0 None -67 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44457002 197875 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
CHEMBL270691 197875 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
44577510 371922 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577523 371922 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 371922 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508068 371922 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
164627532 369874 0 None 18 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 11 3 3 6.1 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4878922 369874 0 None 18 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 11 3 3 6.1 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
137649368 313306 0 None -53 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
137657607 313306 0 None -53 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4078495 313306 0 None -53 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103567 313306 0 None -53 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
122184576 241002 0 None -213 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 241002 0 None -213 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44401313 26557 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1184856 26557 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
11273288 27222 0 None -223 3 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 27222 0 None -223 3 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL410168 488101 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1527 30 20 19 -3.3 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44448631 195446 0 None -44 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 195446 0 None -44 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
178323510 467362 0 None -6 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 759 21 6 6 4.3 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](C(C)C)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6174653 467362 0 None -6 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 759 21 6 6 4.3 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](C(C)C)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
102096778 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
51351151 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
51351277 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
53318437 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
53322400 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
91932359 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
91932360 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL1688110 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL1688111 121590 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2323794 477562 0 None -5 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1685 23 20 21 -0.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137638218 312745 0 None 2 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4071283 312745 0 None 2 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL2372365 485840 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1081 17 13 14 -0.3 C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC(C)(C)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
44408189 333518 0 None -28 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 333518 0 None -28 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL3600840 487199 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2323798 477566 0 None -15 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1607 23 18 21 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCN)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2304248 485328 0 None -2 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 2325 53 32 31 -6.3 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
178319924 466959 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 778 22 8 7 2.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6165084 466959 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 778 22 8 7 2.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
164614821 368565 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 12 3 3 6.9 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4858724 368565 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 12 3 3 6.9 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
178321360 467211 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 695 19 6 6 3.0 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6171209 467211 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 695 19 6 6 3.0 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
45487285 394093 0 None -7 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 627 15 9 7 0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2cc(O)ccc2c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566760 394093 0 None -7 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 627 15 9 7 0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2cc(O)ccc2c1)C(N)=O 10.1016/j.bmcl.2009.07.025
168295131 375277 0 None -15 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 375277 0 None -15 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
137654884 314467 0 None 3 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4092082 314467 0 None 3 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
44408252 277946 0 None -30 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 277946 0 None -30 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
164621683 368882 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 12 3 3 6.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4863711 368882 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 12 3 3 6.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
44441636 194427 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248701 194427 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
46232227 429170 0 None 2 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589517 429170 0 None 2 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL3349030 486807 0 None -14 3 Human 7.3 pEC50 = 7.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
49862375 38937 0 None -69 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 38937 0 None -69 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
164624386 369474 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 10 4 4 5.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4872932 369474 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 10 4 4 5.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL414778 488367 0 None -323 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1578 47 20 20 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL437050 484343 3 None -8 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
71457994 160098 0 None -12 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
CHEMBL2112213 160098 0 None -12 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
44305770 467874 0 None -1 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL62228 467874 0 None -1 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
178317565 466675 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 810 23 8 7 2.8 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6151661 466675 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 810 23 8 7 2.8 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
155542149 347205 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 740 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4520119 347205 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 740 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155549760 347952 0 None -11 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155563222 347952 0 None -11 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539621 347952 0 None -11 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4572994 347952 0 None -11 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155555182 348376 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 778 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550582 348376 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 778 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
118722929 235155 0 None -6 3 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358538 235155 0 None -6 3 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3287329 486719 0 None -1 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 825 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL503449 489009 0 None 1 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 699 18 10 7 -0.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
118722925 235152 0 None -7 3 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358534 235152 0 None -7 3 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
122179552 240092 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
CHEMBL3582446 240092 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
162661397 355373 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162671821 355373 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4765156 355373 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4792291 355373 0 None 2 3 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
127036484 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
1323 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
92432 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL3735690 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL430239 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
162649653 353982 0 None -12 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162673830 353982 0 None -12 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4748317 353982 0 None -12 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4795352 353982 0 None -12 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
127036484 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
1323 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
92432 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
CHEMBL3735690 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
CHEMBL430239 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
CHEMBL438294 488712 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1015 13 10 10 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155547310 347702 0 None 10 2 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 750 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4533593 347702 0 None 10 2 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 750 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155549385 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155560756 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4538225 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4568647 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155556954 348595 0 None -81 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155562237 348595 0 None -81 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4556149 348595 0 None -81 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582276 348595 0 None -81 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
132180599 312503 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
137632948 312503 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4068643 312503 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4072129 312503 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
164618352 367956 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 11 3 3 6.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4849626 367956 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 11 3 3 6.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
137657385 315598 0 None None None Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4105142 315598 0 None None None Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL2112008 485087 0 None -51 3 Human 5.3 pEC50 = 5.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL455826 488913 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 775 20 10 7 1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL321870 486640 0 None 5 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 735 18 9 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
164627732 369762 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 10 3 3 7.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4877232 369762 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 10 3 3 7.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
10210972 26545 0 None -9 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 607 9 3 5 3.5 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1184771 26545 0 None -9 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 607 9 3 5 3.5 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1 10.1016/j.bmcl.2004.10.020
178305998 467042 0 None 5 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 750 21 8 6 2.9 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6167262 467042 0 None 5 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 750 21 8 6 2.9 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
46885711 22386 0 None -169 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 22386 0 None -169 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL2323785 477553 0 None -8 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1646 23 19 21 -1.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
155542040 347191 0 None -131 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155568641 347191 0 None -131 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4519837 347191 0 None -131 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4591394 347191 0 None -131 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4299612 477444 0 None -9 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1610 36 16 19 -5.7 CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/acs.jmedchem.5b01894
137634090 312222 0 None -3 5 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 312222 0 None -3 5 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
178307425 467022 0 None -5 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 816 24 9 7 2.9 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6166557 467022 0 None -5 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 816 24 9 7 2.9 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
44441647 310722 0 None -107 3 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399714 310722 0 None -107 3 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
164609537 367709 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 12 3 3 7.6 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4845842 367709 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 12 3 3 7.6 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
164623182 368908 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 607 11 4 4 5.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4864094 368908 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 607 11 4 4 5.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44359591 65702 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 699 19 8 7 -0.2 CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
CHEMBL140847 65702 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 699 19 8 7 -0.2 CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
44347219 40465 0 None None None Human 6.3 pEC50 = 6.3 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 40465 0 None None None Human 6.3 pEC50 = 6.3 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
44359580 66500 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 713 20 5 7 0.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL141497 66500 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 713 20 5 7 0.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
164621263 368772 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 11 3 3 7.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4862172 368772 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 11 3 3 7.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
137646802 313836 0 None -17 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
137657151 313836 0 None -17 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084671 313836 0 None -17 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102613 313836 0 None -17 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155549385 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155560756 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4538225 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4568647 347882 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162662360 355320 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4764556 355320 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL437050 484343 3 None -8 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL410795 488139 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL437050 484343 3 None -8 4 Human 6.3 pEC50 = 6.3 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm030119t
137657206 315506 0 None -1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103985 315506 0 None -1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL421028 488429 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 761 19 9 7 1.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL138212 484674 0 None 8 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 699 19 8 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O 10.1016/j.bmcl.2003.08.078
145966716 329252 0 None -173 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 329252 0 None -173 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
164613550 368429 0 None 12 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4856539 368429 0 None 12 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
164625589 369028 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 11 3 3 7.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4866151 369028 0 None None None Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 11 3 3 7.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44445082 310359 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 310359 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
137659091 315185 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4100160 315185 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
164615813 368444 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 10 3 3 6.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4856877 368444 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 10 3 3 6.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
164626394 369857 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 11 3 3 6.5 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4878558 369857 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 11 3 3 6.5 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
127036484 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
1323 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
92432 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL3735690 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL430239 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
172445559 387810 0 None -6 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5404193 387810 0 None -6 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC5R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL2115441 485126 0 None -61 4 Human 8.2 pEC50 = 8.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 1095 17 14 12 -1.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL195468 485002 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 812 29 9 7 3.8 CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
127036484 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
1323 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
92432 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL3735690 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL430239 5482 39 None -151 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL214332 485136 29 None -2 8 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
122184499 240967 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 240967 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
164609130 367737 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 595 10 4 4 5.1 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4846261 367737 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 595 10 4 4 5.1 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
164612768 368028 0 None 47 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4850501 368028 0 None 47 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
155561730 349645 0 None -19 2 Mouse 6.2 pEC50 = 6.2 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4581269 349645 0 None -19 2 Mouse 6.2 pEC50 = 6.2 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
137637251 311833 0 None -6 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 820 10 9 8 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4060767 311833 0 None -6 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 820 10 9 8 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
178313797 466584 0 None 1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 774 22 8 7 2.2 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6149486 466584 0 None 1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 774 22 8 7 2.2 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL433296 484340 0 None 1 3 Mouse 7.2 pEC50 = 7.2 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
164622453 369370 0 None 2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4871577 369370 0 None 2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
178318027 466749 0 None -4 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 747 21 6 7 3.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6160082 466749 0 None -4 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 747 21 6 7 3.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
45487286 394430 0 None -10 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568940 394430 0 None -10 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL3600922 487207 0 None 1 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408276 157173 0 None -100 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 157173 0 None -100 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
178312968 466791 0 None None None Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 719 20 6 7 2.3 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6161267 466791 0 None None None Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 719 20 6 7 2.3 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
45487298 394431 0 None -7 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568965 394431 0 None -7 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2323800 477568 0 None -39 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1547 19 16 20 -0.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
164617159 368724 0 None 11 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 545 13 4 4 4.7 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4861482 368724 0 None 11 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 545 13 4 4 4.7 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
44441639 194465 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248893 194465 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL105113 484404 0 None 1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 701 18 11 8 -0.7 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
137662147 315224 0 None -99 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 315224 0 None -99 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
178317212 466287 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 844 25 9 8 2.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6141960 466287 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 844 25 9 8 2.0 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
45487409 393983 0 None -9 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566162 393983 0 None -9 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44441633 194936 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL251735 194936 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
46885907 22356 0 None -104 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1090885 22356 0 None -104 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
178305259 466816 0 None -3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 783 22 6 7 3.5 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6161710 466816 0 None -3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 783 22 6 7 3.5 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
44408173 157068 0 None -125 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 157068 0 None -125 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
164621924 369232 0 None 72 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 10 3 3 5.7 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4869531 369232 0 None 72 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 10 3 3 5.7 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
164627491 369770 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4877442 369770 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
44441642 310455 0 None -52 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 310455 0 None -52 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487418 394331 0 None -8 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 632 17 8 8 0.0 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568341 394331 0 None -8 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 632 17 8 8 0.0 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL227239 485297 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1048 14 9 11 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
137635701 311963 0 None -3 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
137646086 311963 0 None -3 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4062425 311963 0 None -3 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084136 311963 0 None -3 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
178323095 467466 0 None 1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 755 21 6 7 2.9 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6176619 467466 0 None 1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 755 21 6 7 2.9 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
45487410 394524 0 None -21 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569696 394524 0 None -21 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
137642664 313960 0 None -7 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4086346 313960 0 None -7 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL320157 486635 0 None 1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 645 15 7 6 -0.0 CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
137641005 312949 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 858 19 8 6 2.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4073782 312949 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 858 19 8 6 2.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
45487297 394196 0 None -13 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567634 394196 0 None -13 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44441645 194541 0 None -23 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 194541 0 None -23 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487406 393980 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566150 393980 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL65339 489364 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL 548 14 7 5 -0.0 CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL2372570 485877 0 None -691 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 1024 17 13 12 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O 10.1021/jm9017866
CHEMBL2323788 477556 0 None -13 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1569 21 19 20 -1.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
45487414 394368 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568577 394368 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
137644603 314029 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 848 19 9 7 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4087277 314029 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 848 19 9 7 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL322889 486643 0 None 3 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 724 18 10 7 -0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL3600736 484279 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
15602927 313768 0 None -1 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL408398 313768 0 None -1 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL322610 486642 0 None 2 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 811 18 10 7 0.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL501394 488981 0 None -2 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 753 18 10 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
162654633 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162672755 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4754987 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL50056 484368 1 None -8 6 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
137658252 315466 0 None 6 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 868 10 10 9 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4103508 315466 0 None 6 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 868 10 10 9 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
45487290 393872 0 None -22 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565474 393872 0 None -22 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
178306905 467012 0 None -2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 780 23 9 7 2.3 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6166426 467012 0 None -2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 780 23 9 7 2.3 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCCNC(=N)N)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2[C@@H](C)O)cc1 10.1021/acs.jmedchem.4c01556
44401520 28173 0 None -141 2 Human 6.2 pEC50 = 6.2 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1196472 28173 0 None -141 2 Human 6.2 pEC50 = 6.2 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
137661461 315221 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4100584 315221 0 None None None Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
178322314 467016 0 None 3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 752 22 7 8 1.5 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6166472 467016 0 None 3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 752 22 7 8 1.5 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
178318426 466722 0 None 1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 729 21 7 7 2.2 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCO)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6153179 466722 0 None 1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 729 21 7 7 2.2 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCO)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2CCO)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
102096778 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351151 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351277 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318437 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322400 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932359 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932360 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688110 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688111 121590 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
137632394 312202 0 None None None Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4065189 312202 0 None None None Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
178312196 466719 0 None -2 3 Human 4.1 pEC50 = 4.1 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 533 9 1 6 3.9 COCCNC(=O)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cn(C)cn1)C1CCCN(c2cccc(C)c2)C1 10.1021/acs.jmedchem.4c01763
CHEMBL6152956 466719 0 None -2 3 Human 4.1 pEC50 = 4.1 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 533 9 1 6 3.9 COCCNC(=O)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cn(C)cn1)C1CCCN(c2cccc(C)c2)C1 10.1021/acs.jmedchem.4c01763
178317199 466847 0 None 1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 758 21 6 7 2.7 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6162452 466847 0 None 1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 758 21 6 7 2.7 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3C)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
145948912 332260 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 332260 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
122179551 240091 0 None -1 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL3582445 240091 0 None -1 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL2370533 477660 0 None None None Human 7.1 pEC50 = 7.1 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 1538 26 17 20 -2.0 CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL105113 484404 0 None 1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 701 18 11 8 -0.7 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
10864861 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10864861 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10886436 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10952071 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL140108 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL334457 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL342954 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10864861 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -1659 9 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44359589 65107 0 None 3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL140324 65107 0 None 3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
178317242 466429 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 808 24 9 8 1.4 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6145322 466429 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 808 24 9 8 1.4 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL438235 488705 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1668 35 21 20 -1.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
164621414 369059 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4866532 369059 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL104397 484401 0 None 2 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 735 18 9 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
155562846 349188 0 None -6 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4570356 349188 0 None -6 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
178318042 466779 0 None -2 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 787 22 6 7 3.4 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6160926 466779 0 None -2 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 787 22 6 7 3.4 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
178313381 466681 0 None 1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 754 21 8 6 2.7 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCCNC(=N)N)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2C)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6151831 466681 0 None 1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 754 21 8 6 2.7 C[C@@H](O)[C@H]1CN(CCN(CCN2C[C@H](CCCNC(=N)N)N(CCCC3CCCCC3)C2=N)CCN2C(=N)NC[C@@H]2C)C(=N)N1CCc1ccc(F)cc1 10.1021/acs.jmedchem.4c01556
137656521 315577 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 315577 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
178306430 467183 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 840 25 9 8 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6170654 467183 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 840 25 9 8 2.1 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
44401524 28247 0 None -151 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 583 8 4 5 3.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1197052 28247 0 None -151 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 583 8 4 5 3.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
178319083 466814 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 751 21 6 7 2.8 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6161645 466814 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 751 21 6 7 2.8 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(F)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2C(C)C)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL227833 485298 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1009 14 10 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL3349030 486807 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2323792 477560 0 None 1 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1559 21 20 21 -3.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
127047336 277103 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798768 277103 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
10122170 258226 0 None None None Human 7.1 pEC50 = 7.1 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 638 10 3 7 2.2 CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL368008 258226 0 None None None Human 7.1 pEC50 = 7.1 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 638 10 3 7 2.2 CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
178308103 467079 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 790 22 8 6 3.3 C[C@H]1CNC(=N)N1CCN(CCN1C[C@H](CCCNC(=N)N)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
CHEMBL6168212 467079 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 790 22 8 6 3.3 C[C@H]1CNC(=N)N1CCN(CCN1C[C@H](CCCNC(=N)N)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
127036484 5482 39 None -151 7 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
1323 5482 39 None -151 7 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
92432 5482 39 None -151 7 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL3735690 5482 39 None -151 7 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL430239 5482 39 None -151 7 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
155556466 348467 0 None -11 3 Mouse 8.1 pEC50 = 8.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4552764 348467 0 None -11 3 Mouse 8.1 pEC50 = 8.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL501679 488987 0 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 753 18 10 7 0.6 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
46232226 451699 0 None 6 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602853 451699 0 None 6 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589308 489303 0 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 809 22 9 8 -0.3 CC(=O)NCC(=O)N(CC(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmc.2009.12.010
CHEMBL214332 485136 29 None -64 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 485136 29 None -64 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL415200 488390 0 None 5 5 Mouse 8.1 pEC50 = 8.1 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 1053 17 12 14 -1.2 C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
132180598 313735 0 None -7 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
155543031 313735 0 None -7 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4083717 313735 0 None -7 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4522298 313735 0 None -7 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
155556954 348595 0 None -81 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155562237 348595 0 None -81 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4556149 348595 0 None -81 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582276 348595 0 None -81 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44408155 277834 0 None -141 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 277834 0 None -141 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
164609002 367698 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164622957 367698 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4845749 367698 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4871777 367698 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164627764 369830 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 603 11 4 4 4.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4878201 369830 0 None None None Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 603 11 4 4 4.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL3349030 486807 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
122184912 241131 0 None -2 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 241131 0 None -2 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL376339 487561 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 998 13 10 10 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL405282 487855 22 None -245 6 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL411359 488169 0 None -1 4 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1552 47 21 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 487855 22 None -245 6 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
155549302 347880 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155551195 347880 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4538209 347880 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4541098 347880 0 None -4 3 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44305956 202821 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL305132 202821 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
44305784 468363 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 447 8 4 3 3.4 CC1CCN(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL64967 468363 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 447 8 4 3 3.4 CC1CCN(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL2323787 477555 0 None -41 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1672 24 19 21 -0.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137635701 311963 0 None -3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
137646086 311963 0 None -3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4062425 311963 0 None -3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084136 311963 0 None -3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL3600921 487206 0 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44391929 26681 0 None -15 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 571 8 3 5 3.3 CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1185810 26681 0 None -15 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 571 8 3 5 3.3 CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL502300 488996 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1091 16 15 11 -0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL381739 487607 0 None 11 2 Human 6.1 pEC50 = 6.1 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 827 12 9 8 -0.1 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
44408154 278594 0 None -147 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 278594 0 None -147 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL2323797 477565 0 None -44 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1550 19 17 20 -1.0 C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm301253y
10188529 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL365401 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
10188529 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL365401 6967 6 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
45487292 393941 0 None -4 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 628 16 9 8 -0.3 N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565900 393941 0 None -4 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 628 16 9 8 -0.3 N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2323796 477564 0 None -79 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1711 24 20 21 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
24882615 197797 0 None -1 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL270270 197797 0 None -1 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL331259 486767 0 None None None Human 7.1 pEC50 = 7.1 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 936 15 11 9 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
CHEMBL408509 488020 0 None None None Human 6.1 pEC50 = 6.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1627 47 20 19 -0.7 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44401310 27050 0 None -109 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 557 7 4 5 2.9 C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1188043 27050 0 None -109 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 557 7 4 5 2.9 C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
44348144 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None -66 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44441684 194544 0 None -89 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 194544 0 None -89 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
162654633 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162672755 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4754987 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 354516 0 None -18 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL2323795 477563 0 None -19 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1761 23 20 21 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL264190 484234 0 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL2369485 477578 0 None -1 3 Mouse 7.1 pEC50 = 7.1 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1528 24 22 21 -4.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
155549302 347880 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155551195 347880 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4538209 347880 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4541098 347880 0 None -4 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
178318497 466324 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 761 22 7 7 3.0 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6142663 466324 0 None -3 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 761 22 7 7 3.0 Cc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](CCO)N(CCCC4CCCCC4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2Cc2c[nH]cn2)cc1 10.1021/acs.jmedchem.4c01556
155554827 348663 0 None -2 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4557656 348663 0 None -2 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155562993 349246 0 None 1 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 694 14 6 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4571760 349246 0 None 1 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 694 14 6 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137637026 311852 0 None -162 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 311852 0 None -162 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44401321 26071 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1181867 26071 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
102096778 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351151 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351277 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318437 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322400 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932359 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932360 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688110 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688111 121590 0 None -4 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
45487415 394525 0 None -11 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569697 394525 0 None -11 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
164625186 369247 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4869669 369247 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
145973975 329587 0 None -50 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 329587 0 None -50 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
46885480 22073 0 None -63 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 22073 0 None -63 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
45487412 393914 0 None -8 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565740 393914 0 None -8 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
178312876 466739 0 None -2 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 785 23 7 8 2.3 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6159744 466739 0 None -2 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 785 23 7 8 2.3 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H](Cc4c[nH]cn4)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCO)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL430489 488571 0 None 2 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 686 18 9 8 -1.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44391999 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
44392015 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
44441681 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
6918813 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL1187982 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL1196338 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249319 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL368876 27043 2 None -120 4 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL439691 488789 0 None -63 3 Human 7.0 pEC50 = 7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438030 488691 0 None -63 3 Human 7.0 pEC50 = 7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 1551 47 21 18 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
51350911 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351024 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318435 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322399 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932357 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932358 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688106 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688109 121588 0 None -3 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
178319286 467223 0 None -7 3 Mouse 5.0 pEC50 = 5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 765 22 7 7 2.8 N=C1NC[C@H](CCO)N1CCN(CCN1C[C@H](CCO)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
CHEMBL6171552 467223 0 None -7 3 Mouse 5.0 pEC50 = 5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 765 22 7 7 2.8 N=C1NC[C@H](CCO)N1CCN(CCN1C[C@H](CCO)N(CCCC2CCCCC2)C1=N)CCN1C[C@H](Cc2c[nH]cn2)N(CCc2ccc(F)cc2)C1=N 10.1021/acs.jmedchem.4c01556
178313807 466591 0 None -20 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 804 24 9 8 1.6 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
CHEMBL6149598 466591 0 None -20 3 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assayAgonist activity at mouse MC5R expressed in HEK293 cells using ONPG as substrate preincubated with compound for 6 hrs followed by substrate addition by beta-galactosidase cAMP assay
ChEMBL 804 24 9 8 1.6 CCOc1ccc(CCN2C(=N)N(CCN(CCN3C[C@H]([C@@H](C)O)N(CCc4ccc(C)cc4)C3=N)CCN3C(=N)NC[C@@H]3CCO)C[C@@H]2CCCNC(=N)N)cc1 10.1021/acs.jmedchem.4c01556
168277916 373761 0 None None None Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5181812 373761 0 None None None Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168290510 374945 0 None None None Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 374945 0 None None None Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168293710 375204 0 None None None Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 375204 0 None None None Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168278271 374186 0 None None None Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 374186 0 None None None Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168276507 373359 0 None None None Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 373359 0 None None None Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168285101 374705 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 374705 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168273645 373418 0 None None None Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5176443 373418 0 None None None Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168271237 373575 0 None None None Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 373575 0 None None None Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168285904 374731 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 374731 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168294114 375225 0 None None None Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5204285 375225 0 None None None Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168274920 373357 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 373357 0 None None None Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168283616 374306 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 374306 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
11993702 484262 27 None -7079 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 484262 27 None -7079 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
DB11700 484262 27 None -7079 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
168272660 373521 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 373521 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168277543 373759 0 None None None Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 373759 0 None None None Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
10408 1486 31 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 1486 31 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 1486 31 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 1486 31 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 1486 31 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
168289457 374445 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 374445 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168272615 373477 0 None None None Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 373477 0 None None None Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168284256 374020 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 374020 0 None None None Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168271934 373182 0 None None None Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 373182 0 None None None Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
168296647 375502 0 None None None Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 375502 0 None None None Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168270124 373056 0 None None None Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 373056 0 None None None Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
127036484 5482 39 None -10 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
1323 5482 39 None -10 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
92432 5482 39 None -10 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL3735690 5482 39 None -10 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL430239 5482 39 None -10 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
168276294 373595 0 None None None Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179373 373595 0 None None None Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168284733 374685 0 None None None Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 374685 0 None None None Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289404 374377 0 None None None Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 374377 0 None None None Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168277258 373793 0 None None None Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 373793 0 None None None Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168281389 373997 0 None None None Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 373997 0 None None None Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
168277761 373394 0 None None None Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175981 373394 0 None None None Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168295726 375436 0 None None None Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 375436 0 None None None Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168281421 374031 0 None None None Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 374031 0 None None None Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL413573 488288 0 None None None Human 8.7 pKd = 8.7 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 879 13 10 8 1.2 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
44445085 197396 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 197396 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
172445058 387891 0 None None None Mouse 6.0 pKd = 6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5405613 387891 0 None None None Mouse 6.0 pKd = 6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
164610096 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
164620129 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456626 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4852476 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4866219 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5419394 368170 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456058 388500 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5417913 388500 0 None None None Mouse 5.9 pKd = 5.9 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/acs.jmedchem.3c00432
164613676 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
164619641 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172451922 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172463893 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4861645 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4865888 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5406385 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5435335 368738 1 None None None Mouse 5.8 pKd = 5.8 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172443052 387786 0 None None None Mouse 6.7 pKd = 6.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 785 18 9 7 0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5403689 387786 0 None None None Mouse 6.7 pKd = 6.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 785 18 9 7 0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172449584 388013 0 None None None Mouse 6.7 pKd = 6.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5408661 388013 0 None None None Mouse 6.7 pKd = 6.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172440979 387523 0 None None None Mouse 5.7 pKd = 5.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 814 19 9 7 0.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5397924 387523 0 None None None Mouse 5.7 pKd = 5.7 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 814 19 9 7 0.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.3c00432
164613676 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
164619641 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172451922 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172463893 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4861645 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4865888 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5406385 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5435335 368738 1 None None None Mouse 6.6 pKd = 6.6 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
122178167 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
132938008 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
137638391 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL3577996 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4071633 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4102048 239867 0 None None None Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
155561116 349002 0 None None None Mouse 6.5 pKd = 6.5 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 349002 0 None None None Mouse 6.5 pKd = 6.5 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
122184635 241007 0 None None None Human 7.4 pKd = 7.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None None None Human 7.4 pKd = 7.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
162650385 353953 0 None None None Mouse 7.4 pKd = 7.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4747952 353953 0 None None None Mouse 7.4 pKd = 7.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL3577981 487140 1 None None None Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 10 10 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
171378453 388656 0 None None None Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 799 19 9 7 0.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5421386 388656 0 None None None Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 799 19 9 7 0.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL3577981 487140 1 None None None Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 976 12 10 10 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
44577514 336975 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577515 336975 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 336975 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 336975 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
122178167 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
132938008 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
137638391 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL3577996 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4071633 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4102048 239867 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
164610096 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
164620129 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456626 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4852476 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4866219 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5419394 368170 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172452729 388263 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 771 17 9 7 -0.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413452 388263 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 771 17 9 7 -0.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CN)C(N)=O 10.1021/acs.jmedchem.3c00432
155544852 348969 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 348969 0 None None None Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
172447220 387427 0 None None None Mouse 7.2 pKd = 7.2 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase incubated in presence of MTII (Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2) by schild analysisAntagonist activity at mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase incubated in presence of MTII (Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2) by schild analysis
ChEMBL 1099 17 12 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cn(C)cn2)NC1=O 10.1021/acs.jmedchem.3c00432
CHEMBL5396011 387427 0 None None None Mouse 7.2 pKd = 7.2 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase incubated in presence of MTII (Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2) by schild analysisAntagonist activity at mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase incubated in presence of MTII (Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2) by schild analysis
ChEMBL 1099 17 12 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cn(C)cn2)NC1=O 10.1021/acs.jmedchem.3c00432
162645080 353341 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4740561 353341 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
172449408 388260 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172449794 388260 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413381 388260 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5414015 388260 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172449003 388268 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 842 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(N)=O)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413535 388268 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysisAntagonist activity at mouse MC5R expressed in HEK293 cells assessed as reduction in NDP-MSH induced cAMP formation incubated for 2 hrs by AlphaScreen based schild plot analysis
ChEMBL 842 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(N)=O)C(N)=O 10.1021/acs.jmedchem.3c00432
155548853 347886 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 347886 0 None None None Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
122194229 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
1324 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
16197727 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
4836 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL3629347 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL441738 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
DB04931 621 23 None -4 9 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
122194229 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
1324 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
16197727 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
4836 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL3629347 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL441738 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
DB04931 621 23 None -5 7 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
1341 6264 0 None 6 3 Human 10.5 pIC50 None 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1335 647 0 None -630 3 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9892020
O00253 647 0 None -630 3 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9892020
1342 509 0 None None None Human 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12904077
122194229 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
1324 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
16197727 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
4836 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
CHEMBL3629347 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
CHEMBL441738 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
DB04931 621 23 None -5 7 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 12007532
127036484 5482 39 None -10 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 12007532
1323 5482 39 None -10 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 12007532
92432 5482 39 None -10 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 12007532
CHEMBL3735690 5482 39 None -10 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 12007532
CHEMBL430239 5482 39 None -10 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 12007532


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

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44366081 24554 0 None None None Human 10.5 pEC50 = 10.5 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 24554 0 None None None Human 10.5 pEC50 = 10.5 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
127036484 5482 39 None None None Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm049010r
1323 5482 39 None None None Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm049010r
92432 5482 39 None None None Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm049010r
CHEMBL3735690 5482 39 None None None Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm049010r
CHEMBL430239 5482 39 None None None Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm049010r
122194229 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
1324 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
16197727 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
4836 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
CHEMBL3629347 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
CHEMBL441738 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
DB04931 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm020296e
122194229 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
1324 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
16197727 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
4836 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
CHEMBL3629347 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
CHEMBL441738 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
DB04931 621 23 None None None Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0104872
101176453 366336 0 None None None Human 10.1 pEC50 = 10.1 Binding
Agonist activity at human melanocortin receptor 5Agonist activity at human melanocortin receptor 5
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL4792986 366336 0 None None None Human 10.1 pEC50 = 10.1 Binding
Agonist activity at human melanocortin receptor 5Agonist activity at human melanocortin receptor 5
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL1161322 484166 0 None None None Human 10.1 pEC50 = 10.1 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1034 15 12 10 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
122194229 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
1324 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
16197727 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
4836 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
CHEMBL3629347 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
CHEMBL441738 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
DB04931 621 23 None None None Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049010r
CHEMBL2096742 484199 0 None None None Human 9.9 pEC50 = 9.9 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
CHEMBL442504 484358 0 None None None Human 9.9 pEC50 = 9.9 Binding
Signal transduction efficacy in cAMP assay in CHO cells expressing human melanocortin receptor 5Signal transduction efficacy in cAMP assay in CHO cells expressing human melanocortin receptor 5
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
127036484 5482 39 None None None Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm020296e
1323 5482 39 None None None Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm020296e
92432 5482 39 None None None Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm020296e
CHEMBL3735690 5482 39 None None None Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm020296e
CHEMBL430239 5482 39 None None None Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm020296e
44327392 279054 0 None None None Mouse 9.8 pEC50 = 9.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1025 21 12 12 -0.6 CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0104872
CHEMBL386583 279054 0 None None None Mouse 9.8 pEC50 = 9.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1025 21 12 12 -0.6 CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0104872
CHEMBL1161323 484441 0 None None None Human 9.7 pEC50 = 9.7 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1116 15 12 10 2.6 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL214332 485136 29 None None None Mouse 9.5 pEC50 = 9.5 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049010r
CHEMBL2369959 477614 0 None None None Mouse 9.4 pEC50 = 9.4 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1486 23 19 18 -2.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL214332 485136 29 None None None Mouse 9.4 pEC50 = 9.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm020296e
CHEMBL214332 485136 29 None None None Mouse 9.4 pEC50 = 9.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0104872
CHEMBL2369967 477622 0 None None None Mouse 9.3 pEC50 = 9.3 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1420 21 18 17 -2.7 C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
127036484 5482 39 None None None Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500340z
1323 5482 39 None None None Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500340z
92432 5482 39 None None None Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500340z
CHEMBL3735690 5482 39 None None None Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500340z
CHEMBL430239 5482 39 None None None Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500340z
CHEMBL2369964 477619 0 None None None Mouse 9.0 pEC50 = 9.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1497 23 18 18 -2.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44322868 215692 0 None None None Human 9.0 pEC50 = 9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 215692 0 None None None Human 9.0 pEC50 = 9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL2369963 477618 0 None None None Mouse 8.7 pEC50 = 8.7 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1497 23 18 18 -2.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL1161318 484438 0 None None None Human 8.0 pEC50 = 8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1062 15 13 10 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
CHEMBL347364 487104 0 None None None Mouse 7.0 pEC50 = 7 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 722 19 8 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
CHEMBL191063 484980 0 None None None Mouse 7.0 pEC50 = 7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL365794 487359 0 None None None Mouse 6.0 pEC50 = 6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
11038873 79296 0 None None None Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
11763303 79296 0 None None None Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL14416 79296 0 None None None Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL446941 79296 0 None None None Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
10260053 332923 0 None None None Human 6.0 pEC50 = 6.0 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 332923 0 None None None Human 6.0 pEC50 = 6.0 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL347216 487103 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
CHEMBL190080 484964 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 932 31 10 10 -0.8 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL275303 484244 0 None None None Mouse 4.9 pEC50 = 4.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 707 15 7 6 0.9 CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL432027 488582 0 None None None Mouse 5.9 pEC50 = 5.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 734 18 9 6 1.2 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
46877881 465190 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 465190 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL94391 484388 0 None None None Mouse 6.9 pEC50 = 6.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL327479 486702 0 None None None Mouse 6.8 pEC50 = 6.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 695 18 8 6 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL433522 488591 0 None None None Mouse 4.8 pEC50 = 4.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 647 18 8 8 -1.7 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccncc1)C(N)=O 10.1021/jm020296e
CHEMBL190551 484968 0 None None None Mouse 7.8 pEC50 = 7.8 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 10 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL348901 487107 0 None None None Mouse 6.8 pEC50 = 6.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 722 19 8 7 0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
44323234 40519 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347221 40519 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL124169 40519 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 40519 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL1161321 484440 0 None None None Human 7.8 pEC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1096 15 13 10 1.3 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
CHEMBL2371147 485690 0 None None None Mouse 6.8 pEC50 = 6.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 672 16 8 7 -0.7 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
CHEMBL3422431 487062 0 None None None Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 821 18 9 6 1.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/ml500340z
118735609 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
118735610 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422432 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422433 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL190953 484978 0 None None None Mouse 5.7 pEC50 = 5.7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL372237 487489 0 None None None Mouse 5.7 pEC50 = 5.7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2372589 484227 0 None None None Human 8.7 pEC50 = 8.7 Binding
Activity of cyclic alpha MSH analogues at human melanocortin receptor Melanocortin 5 receptorActivity of cyclic alpha MSH analogues at human melanocortin receptor Melanocortin 5 receptor
ChEMBL 1096 15 12 10 1.6 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
171355776 386645 0 None None None Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human melanocortin receptor 5Agonist activity at human melanocortin receptor 5
ChEMBL 1096 15 12 10 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2Cc3ccccc3CN2C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL5282523 386645 0 None None None Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human melanocortin receptor 5Agonist activity at human melanocortin receptor 5
ChEMBL 1096 15 12 10 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2Cc3ccccc3CN2C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL2369969 477624 0 None None None Mouse 8.7 pEC50 = 8.7 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1401 19 17 17 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2096742 484199 0 None None None Mouse 8.6 pEC50 = 8.6 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm049010r
CHEMBL2369973 477628 0 None None None Mouse 8.6 pEC50 = 8.6 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1612 23 19 18 -2.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
127035019 7320 11 None None None Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/ml500340z
1325 7320 11 None None None Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/ml500340z
9898183 7320 11 None None None Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/ml500340z
CHEMBL3422426 7320 11 None None None Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/ml500340z
CHEMBL3735607 7320 11 None None None Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/ml500340z
118735609 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
118735610 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422432 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422433 237667 0 None None None Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
44269217 63908 0 None None None Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL13910 63908 0 None None None Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL2369974 477629 0 None None None Mouse 7.7 pEC50 = 7.7 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1536 23 19 18 -1.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL329490 486725 0 None None None Mouse 5.7 pEC50 = 5.7 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 745 18 8 6 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
118735606 237666 0 None None None Mouse 4.6 pEC50 = 4.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 877 18 9 7 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL3422429 237666 0 None None None Mouse 4.6 pEC50 = 4.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 877 18 9 7 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/ml500340z
11828678 474738 0 None None None Mouse 5.6 pEC50 = 5.6 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 721 16 8 6 1.0 CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm0104872
CHEMBL96531 474738 0 None None None Mouse 5.6 pEC50 = 5.6 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 721 16 8 6 1.0 CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm0104872
CHEMBL2096745 485068 0 None None None Mouse 4.6 pEC50 = 4.6 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 658 15 7 7 -0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/jm020296e
CHEMBL191120 484981 0 None None None Mouse 6.6 pEC50 = 6.6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL370321 487484 0 None None None Mouse 6.6 pEC50 = 6.6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44269214 198760 0 None None None Human 5.6 pEC50 = 5.6 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276012 198760 0 None None None Human 5.6 pEC50 = 5.6 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
118735604 237664 0 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL3422427 237664 0 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL329847 486729 0 None None None Mouse 5.5 pEC50 = 5.5 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 695 18 8 6 0.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2369982 477633 0 None None None Mouse 8.5 pEC50 = 8.5 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1536 23 19 18 -1.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369960 477615 0 None None None Mouse 8.5 pEC50 = 8.5 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1496 23 18 17 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2370154 477645 0 None None None Human 8.5 pEC50 = 8.5 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 1038 17 14 11 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
CHEMBL2369965 477620 0 None None None Mouse 8.5 pEC50 = 8.5 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1523 24 18 18 -1.6 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44369234 98529 0 None None None Mouse 8.4 pEC50 = 8.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL152612 98529 0 None None None Mouse 8.4 pEC50 = 8.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL264190 484234 0 None None None Mouse 8.4 pEC50 = 8.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL330233 486737 0 None None None Mouse 6.5 pEC50 = 6.5 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 619 16 8 6 -0.5 CC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL365913 487361 0 None None None Mouse 7.5 pEC50 = 7.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 12 10 -1.5 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL188738 484961 0 None None None Mouse 6.5 pEC50 = 6.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL189991 484963 0 None None None Mouse 5.5 pEC50 = 5.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2369976 477631 0 None None None Mouse 5.5 pEC50 = 5.5 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1427 19 16 17 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL154153 484178 0 None None None Mouse 7.5 pEC50 = 7.5 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL264190 484234 0 None None None Mouse 7.5 pEC50 = 7.5 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL350012 487113 0 None None None Mouse 4.4 pEC50 = 4.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 636 18 9 8 -2.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm020296e
CHEMBL96871 484389 0 None None None Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 707 15 7 6 0.9 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL431092 488573 0 None None None Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 751 18 8 7 1.9 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2371150 485691 0 None None None Mouse 4.4 pEC50 = 4.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 570 16 8 7 -2.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm020296e
CHEMBL1161320 484439 0 None None None Human 6.4 pEC50 = 6.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1020 15 13 10 0.3 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
44269189 198615 0 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL275067 198615 0 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL190203 484966 0 None None None Mouse 5.4 pEC50 = 5.4 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL264190 484234 0 None None None Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL357558 487134 0 None None None Mouse 8.3 pEC50 = 8.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
CHEMBL2369983 477634 0 None None None Mouse 8.3 pEC50 = 8.3 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1486 23 19 18 -2.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL330561 486739 0 None None None Mouse 7.4 pEC50 = 7.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 701 18 8 7 0.8 CC(=O)N[C@@H](Cc1cccs1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL317969 486618 0 None None None Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
44347840 317432 0 None None None Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 317432 0 None None None Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 317432 0 None None None Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL2369966 477621 0 None None None Mouse 7.4 pEC50 = 7.4 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1459 21 17 18 -3.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369961 477616 0 None None None Mouse 6.4 pEC50 = 6.4 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1522 21 18 17 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCc3ccccc3C2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44269246 81940 11 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
9915813 81940 11 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
CHEMBL14642 81940 11 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
CHEMBL275042 81940 11 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
CHEMBL1161316 484437 0 None None None Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1048 15 13 10 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
10101361 311638 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL405174 311638 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL151906 484709 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 702 18 8 8 0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL154251 484715 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 646 18 8 7 -1.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL2369975 477630 0 None None None Mouse 8.3 pEC50 = 8.3 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1562 24 19 18 -1.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369970 477625 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1371 21 18 18 -4.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2371832 485779 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL432201 488584 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 734 18 9 6 1.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
44366171 239900 0 None None None Human 6.3 pEC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 239900 0 None None None Human 6.3 pEC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL3422430 487061 0 None None None Mouse 5.3 pEC50 = 5.3 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 833 15 8 6 1.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/ml500340z
44322795 473859 0 None None None Human 6.3 pEC50 = 6.3 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 473859 0 None None None Human 6.3 pEC50 = 6.3 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL94369 489411 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 745 18 8 6 1.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2371835 485781 0 None None None Mouse 7.2 pEC50 = 7.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL186970 484956 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 861 28 10 10 -0.9 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2371829 485778 0 None None None Mouse 5.2 pEC50 = 5.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL2371833 485780 0 None None None Mouse 5.2 pEC50 = 5.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.7 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
44323020 333622 0 None None None Human 6.2 pEC50 = 6.2 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 333622 0 None None None Human 6.2 pEC50 = 6.2 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL320157 486635 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 645 15 7 6 -0.0 CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2369968 477623 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1410 21 19 18 -4.0 C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm049010r
CHEMBL2369971 477626 0 None None None Mouse 8.1 pEC50 = 8.1 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1446 21 17 17 -2.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2096693 485066 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 658 15 7 7 -0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/jm020296e
CHEMBL2369962 477617 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1397 21 17 18 -4.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL152555 484710 0 None None None Mouse 5.2 pEC50 = 5.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 722 19 8 7 0.5 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL358833 487188 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 722 19 8 7 0.5 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL346925 484278 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
118735605 237665 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 897 19 9 6 3.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/ml500340z
CHEMBL3422428 237665 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 897 19 9 6 3.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/ml500340z
CHEMBL2369972 477627 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1436 21 18 18 -3.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL373344 487492 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL188459 484959 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190102 484965 0 None None None Mouse 5.1 pEC50 = 5.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -0.9 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)Cc1ccccc1 10.1021/jm0490033
CHEMBL2369977 477632 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL 1458 23 18 18 -1.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL349795 487111 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 652 18 8 8 -1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccs1)C(N)=O 10.1021/jm020296e
CHEMBL152986 484712 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 646 18 8 7 -1.1 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL317968 486617 0 None None None Mouse 7.0 pEC50 = 7.0 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 696 18 8 7 0.1 CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
11813437 198793 0 None None None Human 5.0 pEC50 = 5.0 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276301 198793 0 None None None Human 5.0 pEC50 = 5.0 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL2371147 485690 0 None None None Mouse 6.0 pEC50 = 6.0 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 672 16 8 7 -0.7 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
44366081 24554 0 None None None Human 10.6 pIC50 = 10.6 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 24554 0 None None None Human 10.6 pIC50 = 10.6 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161322 484166 0 None None None Human 10.5 pIC50 = 10.5 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1034 15 12 10 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 484199 0 None None None Human 10.1 pIC50 = 10.1 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
16049796 174469 0 None None None Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 543 11 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL220018 174469 0 None None None Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 543 11 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
44418438 327605 0 None None None Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL425442 327605 0 None None None Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL1161323 484441 0 None None None Human 10.0 pIC50 = 10.0 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1116 15 12 10 2.6 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL2371966 485796 0 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1015 12 8 9 2.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
44418413 164627 0 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 500 11 2 3 4.7 O=C(CCc1c[nH]c2ccccc12)NCCCCCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218558 164627 0 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 500 11 2 3 4.7 O=C(CCc1c[nH]c2ccccc12)NCCCCCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
44418437 164589 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL218361 164589 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL501592 488985 0 None None None Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1091 16 15 11 -0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2371962 485793 0 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1055 14 10 10 2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
44418420 279130 0 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL387169 279130 0 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
122194229 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
1324 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
16197727 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
4836 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL3629347 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL441738 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
DB04931 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
122194229 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
1324 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
16197727 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
4836 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL3629347 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL441738 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
DB04931 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
122194229 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
1324 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
16197727 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
4836 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL3629347 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL441738 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
DB04931 621 23 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL2096742 484199 0 None None None Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm801300c
CHEMBL2371968 477721 0 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1069 12 8 9 4.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL524861 489128 0 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1041 16 15 11 -2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2372589 484227 0 None None None Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1096 15 12 10 1.6 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL204310 485035 0 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 908 15 11 9 -0.2 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0510326
127036484 5482 39 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
1323 5482 39 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
92432 5482 39 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL3735690 5482 39 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL430239 5482 39 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL2371965 477720 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1055 12 8 9 3.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
71449048 160026 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456220 160026 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 160026 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 160026 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL203760 485032 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 877 12 9 8 1.0 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0510326
CHEMBL446185 488874 0 None None None Human 7.0 pIC50 = 7 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 867 14 11 9 -0.6 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
CHEMBL1775062 484790 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 992 15 15 10 -1.6 C[C@@H]1NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
137659790 315167 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 315167 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190551 484968 0 None None None Mouse 6.0 pIC50 = 6 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 10 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL408509 488020 0 None None None Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1627 47 20 19 -0.7 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL5077811 478706 0 None None None Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1073 16 14 13 -1.6 CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL372237 487489 0 None None None Mouse 5.0 pIC50 = 5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
44396987 139478 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL187774 139478 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
122184912 241131 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 241131 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44397220 327654 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 327654 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL264190 484234 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL264190 484234 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 685 18 10 7 -0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.2c01794
CHEMBL2096759 485069 0 None None None Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1567 47 21 20 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44408287 157053 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 157053 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL427205 488473 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 829 13 10 8 0.0 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
49862378 38940 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 38940 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
15953833 160466 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 160466 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
137647538 313847 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 313847 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137646617 313441 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 313441 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL5085972 477477 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL3601426 487208 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL214332 485136 29 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL1161321 484440 0 None None None Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1096 15 13 10 1.3 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
145976444 328925 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 328925 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
24774521 310316 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398635 310316 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44397652 251710 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL361883 251710 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
155546131 347623 0 None None None Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4531291 347623 0 None None None Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
6918276 39502 6 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 39502 6 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
46919520 39036 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 39036 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44431512 292638 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 292638 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL5092761 479551 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1987 26 22 22 0.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3577981 487140 1 None None None Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 976 12 10 10 -1.2 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL188738 484961 0 None None None Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL5087814 479290 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1859 20 19 19 1.7 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44448660 195354 0 None None None Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 195354 0 None None None Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
122184578 241004 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600839 241004 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44577514 336975 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577515 336975 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 336975 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 336975 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
49862375 38937 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 38937 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
54586246 123581 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762008 123581 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL376339 487561 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 998 13 10 10 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44277696 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44372933 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
70695694 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL2111251 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL349298 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44391999 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44277696 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
44372933 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
70695694 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL2111251 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL349298 159974 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
118735103 237591 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 237591 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
122194229 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
1324 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
16197727 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
4836 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
CHEMBL3629347 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
CHEMBL441738 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
DB04931 621 23 None None None Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.9b00860
54584301 123574 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
CHEMBL1761872 123574 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
10483153 123575 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 123575 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
54584302 123576 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 123576 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
44397461 254200 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 254200 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL3350396 486875 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1095 17 14 12 -1.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
15953838 135872 0 None None None Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 135872 0 None None None Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
122184575 241001 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 241001 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44408252 277946 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 277946 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
127053937 295732 0 None None None Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL3942822 295732 0 None None None Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL2371964 485795 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1041 14 10 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
57854102 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57854192 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
44348144 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
122184909 241127 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 241127 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5081077 478899 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1983 30 28 23 -3.8 CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168282779 374239 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5188894 374239 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
10864861 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None None None Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL190203 484966 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL365794 487359 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL3600920 487205 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44347840 317432 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 317432 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 317432 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL1161316 484437 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1048 15 13 10 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
CHEMBL3600840 487199 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600832 487195 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145973975 329587 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 329587 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408189 333518 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 333518 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL3349030 486807 0 None None None Human 5.8 pIC50 = 5.8 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5090670 479443 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1872 25 25 21 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137636965 312140 0 None None None Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 312140 0 None None None Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145964837 329293 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 329293 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL5087859 479294 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1966 27 24 22 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
118735100 237588 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 237588 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3600913 487204 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5090946 479450 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1827 23 24 21 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445085 197396 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 197396 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44408173 157068 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 157068 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44408276 157173 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 157173 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
122178167 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
132938008 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
137638391 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL3577996 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4071633 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4102048 239867 0 None None None Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
2044 331721 54 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 331721 54 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 331721 54 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
DB01229 331721 54 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
168296790 375378 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5206941 375378 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5075712 478591 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1924 27 27 22 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5077095 478670 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1938 27 26 22 -1.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3601431 487209 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077144 478676 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1823 25 25 22 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL214332 485136 29 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 485136 29 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44408190 197247 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 197247 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44348144 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44577510 371922 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577523 371922 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 371922 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508068 371922 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44408154 278594 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 278594 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL3349030 486807 0 None None None Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
42630327 311799 1 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 311799 1 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
11993702 484262 27 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 484262 27 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
DB11700 484262 27 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
10408 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
10408 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 1486 31 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL5083551 479049 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1853 23 23 21 -1.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5091236 479464 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1980 28 24 22 -1.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190427 484967 0 None None None Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL190732 484969 0 None None None Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 8 10 -1.3 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL191063 484980 0 None None None Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2371835 485781 0 None None None Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
168273822 373658 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 373658 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL2371712 485760 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1588 44 18 19 -0.8 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2371971 485800 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1051 13 9 9 3.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O 10.1021/jm0614275
CHEMBL502300 488996 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1091 16 15 11 -0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
122194229 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
1324 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
16197727 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
4836 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL3629347 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL441738 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
DB04931 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
122194229 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
1324 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
16197727 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
4836 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL3629347 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL441738 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
DB04931 621 23 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL413573 488288 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 879 13 10 8 1.2 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
CHEMBL204263 485034 0 None None None Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 937 16 12 9 -0.4 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL425591 488459 0 None None None Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 917 14 11 9 0.5 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
CHEMBL503229 489006 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1593 48 23 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL443071 488858 0 None None None Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1609 48 21 20 -2.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL500743 488968 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1041 16 15 11 -2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2371967 485797 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1077 12 8 9 3.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
122184637 241009 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 241009 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371963 485794 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1001 12 8 9 2.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
145973779 329656 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217528 329656 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408155 277834 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 277834 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL439691 488789 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1567 47 21 20 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44347927 313181 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 313181 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL1201469 38416 0 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL5076315 478624 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1948 22 21 19 2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44448590 195963 0 None None None Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 195963 0 None None None Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44417555 197553 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 896 15 9 10 1.2 CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm060768f
CHEMBL268684 197553 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 896 15 9 10 1.2 CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm060768f
CHEMBL2372588 485878 0 None None None Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1082 15 12 10 1.6 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
145967155 329191 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4211275 329191 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408388 277611 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 277611 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
24774519 195242 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253788 195242 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL509582 489086 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1072 14 13 11 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44408275 157086 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 157086 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL409144 488047 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 895 14 11 9 0.0 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm0510326
CHEMBL437050 484343 3 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL3600841 487200 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1800 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2247 1042 63 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
127036484 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
1323 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
92432 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL3735690 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL430239 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
24774438 195243 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253789 195243 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
6918849 241525 0 None None None Human 7.6 pIC50 = 7.6 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360818 241525 0 None None None Human 7.6 pIC50 = 7.6 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2371973 477723 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1083 13 8 9 3.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL2115441 485126 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1095 17 14 12 -1.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
44391999 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
16725559 195368 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 195368 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
10077258 38929 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 38929 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL389674 487742 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 964 13 10 10 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL437050 484343 3 None None None Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
137659790 315167 0 None None None Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 315167 0 None None None Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
122184914 241132 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 241132 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
127036484 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
1323 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
92432 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL3735690 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL430239 5482 39 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL228194 485299 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 995 13 10 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44348144 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
1016 8173 46 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL6067481 479736 0 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
122184635 241007 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5091245 479465 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1911 26 24 22 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445083 310362 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 310362 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600834 487197 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
155544852 348969 0 None None None Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 348969 0 None None None Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL426756 488470 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1004 13 11 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44348200 315941 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 315941 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
44448631 195446 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 195446 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
49862425 38958 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 38958 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
137631599 312447 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 312447 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
2750 64617 55 None None None Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
6604850 64617 55 None None None Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL1398683 64617 55 None None None Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 64617 55 None None None Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
DB09201 64617 55 None None None Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
44431511 178928 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL234629 178928 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
155548853 347886 0 None None None Mouse 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 347886 0 None None None Mouse 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL414778 488367 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1578 47 20 20 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3600833 487196 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413439 488283 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1602 47 21 18 -1.3 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL204864 485037 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 893 15 10 8 1.7 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
168278924 374139 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 374139 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
127053935 290942 0 None None None Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 290942 0 None None None Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3752534 487533 1 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1131 15 12 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1775066 484791 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 992 15 15 10 -1.6 C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
CHEMBL382369 487619 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 859 15 11 9 -0.8 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
CHEMBL5075506 478577 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1925 26 23 22 -0.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
10282847 241526 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360819 241526 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
127053935 290942 0 None None None Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 290942 0 None None None Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
71459938 160473 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 160473 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL189991 484963 0 None None None Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL275999 486330 0 None None None Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL370321 487484 0 None None None Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
10864861 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10886436 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10952071 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
1338 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
9938402 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL140108 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL334457 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL339053 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL342954 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10864861 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10886436 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10952071 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL140108 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL334457 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL342954 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10864861 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL437050 484343 3 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
10210964 139528 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL187990 139528 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL405282 487855 22 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44577519 371951 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
44577520 371951 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL505536 371951 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 371951 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL376614 487569 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1009 14 10 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL405282 487855 22 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL3600843 487202 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 486807 0 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44206252 293235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57853943 293235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3922633 293235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3945076 293235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL227239 485297 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1048 14 9 11 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155561116 349002 0 None None None Mouse 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 349002 0 None None None Mouse 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
145990599 331665 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 331665 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
118735102 237590 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 237590 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
2683 202943 22 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 202943 22 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
DB11073 202943 22 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
24858481 372267 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 909 12 10 10 2.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL510234 372267 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 909 12 10 10 2.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
145971389 329563 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 329563 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
11249545 138497 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 138497 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11364326 138975 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 138975 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL5094168 479635 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1994 29 24 22 -0.7 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
122184638 241010 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 241010 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
25444 311590 1 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL404811 311590 1 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
122184636 241008 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 241008 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL375947 487549 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 964 13 10 10 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
8447 372118 60 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 372118 60 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
DB14201 372118 60 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3198 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL371610 487487 0 None None None Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 8 10 -1.4 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
127036484 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
1323 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
92432 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL3735690 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL430239 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
172445559 387810 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5404193 387810 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL1161320 484439 0 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1020 15 13 10 0.3 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
44422999 333494 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 333494 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
127036484 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
1323 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
92432 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
CHEMBL3735690 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
CHEMBL430239 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/ml500436s
127036484 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
1323 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
92432 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL3735690 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL430239 5482 39 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
163196518 375167 5 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 375167 5 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL1161318 484438 0 None None None Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1062 15 13 10 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
44397455 251902 0 None None None Human 7.4 pIC50 = 7.4 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL362523 251902 0 None None None Human 7.4 pIC50 = 7.4 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
171378344 387423 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 765 15 10 7 0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5395890 387423 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC5R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 765 15 10 7 0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL381739 487607 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 827 12 9 8 -0.1 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
57854102 295005 0 None None None Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57854192 295005 0 None None None Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 295005 0 None None None Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 295005 0 None None None Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
137641157 312974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137655905 312974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 312974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 312974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137640703 313008 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 313008 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
168272745 373610 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccc(cc2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179534 373610 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccc(cc2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
122184911 241129 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 241129 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
127036484 5482 39 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
1323 5482 39 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
92432 5482 39 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
CHEMBL3735690 5482 39 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
CHEMBL430239 5482 39 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm960845e
9808801 123573 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 123573 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL383250 487626 0 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 909 15 11 9 0.4 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
145966490 329307 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 329307 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
24857886 311234 0 None None None Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402769 311234 0 None None None Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
2436 470362 35 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
68617 470362 35 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 470362 35 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
DB01104 470362 35 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
145980719 331313 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 331313 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
168274393 373202 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5172938 373202 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11341045 138459 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 138459 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL3600835 487198 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL438920 488753 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1578 47 20 20 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2371970 485799 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1057 13 9 9 3.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C2CCCCC2)NC1=O 10.1021/jm0614275
CHEMBL438294 488712 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1015 13 10 10 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL203602 485031 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 858 15 11 9 -1.4 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
44206252 293235 0 None None None Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57853943 293235 0 None None None Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3922633 293235 0 None None None Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3945076 293235 0 None None None Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL190080 484964 0 None None None Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 932 31 10 10 -0.8 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2371828 485777 0 None None None Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)C(C)=O 10.1021/jm0490033
168273291 373619 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179637 373619 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5080784 478889 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1887 23 23 21 -0.9 C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445084 316349 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL411391 316349 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
11341046 139167 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 139167 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
11237444 255419 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 255419 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
10304776 160471 0 None None None Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2113041 160471 0 None None None Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
54587278 123582 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 123582 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
44366171 239900 0 None None None Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 239900 0 None None None Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL410795 488139 0 None None None Human 6.3 pIC50 = 6.3 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5080489 478873 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1811 21 23 21 -2.2 C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263948 486113 2 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 1664 50 22 22 -4.7 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960840h
CHEMBL214332 485136 29 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
57854102 295005 0 None None None Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57854192 295005 0 None None None Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 295005 0 None None None Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 295005 0 None None None Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
24858479 337123 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 915 10 10 10 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL449124 337123 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 915 10 10 10 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
57854102 295005 0 None None None Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57854192 295005 0 None None None Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 295005 0 None None None Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 295005 0 None None None Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3349030 486807 0 None None None Human 5.2 pIC50 = 5.2 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL3600922 487207 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24858629 390311 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL552520 390311 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
137660993 315289 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 315289 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
101043845 332258 1 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
145948876 332258 1 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 332258 1 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5177536 332258 1 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5078687 478768 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1853 23 23 21 -1.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL455070 488908 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1022 14 13 11 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
122184634 241006 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 241006 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
122184576 241002 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 241002 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
122184499 240967 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 240967 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600912 487203 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184633 241005 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 241005 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600736 484279 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
49862377 38939 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 38939 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
145976863 328725 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 328725 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408253 277631 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 277631 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
11477853 139182 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 139182 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL5094215 479637 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1825 23 21 21 -0.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190953 484978 0 None None None Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL364711 487350 0 None None None Mouse 5.2 pIC50 = 5.2 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
118735099 237587 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 237587 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL411359 488169 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1552 47 21 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
10304547 327719 0 None None None Human 7.2 pIC50 = 7.2 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL433764 327719 0 None None None Human 7.2 pIC50 = 7.2 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL11359 24083 0 None None None Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
10188529 6967 6 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 6967 6 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 6967 6 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 6967 6 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL365401 6967 6 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
44448629 327664 0 None None None Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 327664 0 None None None Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2310901 485337 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 1523 44 18 17 -1.2 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
10257242 38928 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 38928 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
137636677 312024 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 312024 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44448479 308745 0 None None None Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 308745 0 None None None Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL5090285 479421 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1862 25 26 22 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263822 486104 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 886 16 12 9 -1.6 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
168295131 375277 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 375277 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
71456245 160468 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 160468 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
127036484 5482 39 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
1323 5482 39 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
92432 5482 39 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL3735690 5482 39 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL430239 5482 39 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL2371969 485798 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1017 13 9 9 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0614275
CHEMBL393075 487766 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1032 16 14 11 -0.1 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm070461w
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm060768f
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm801300c
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/jm0510326
11375764 138978 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 138978 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL380638 487587 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL 843 15 10 8 0.6 CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
118735101 237589 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 237589 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL2371972 477722 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1081 12 8 9 4.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](CC2CCC(C3CCCCC3)CC2)NC(=O)[C@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
137641157 312974 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137655905 312974 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 312974 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 312974 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137653925 314477 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 314477 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL2112008 485087 0 None None None Human 5.2 pIC50 = 5.2 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5093939 477486 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
71449048 160026 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456220 160026 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 160026 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 160026 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
137660671 315069 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 315069 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44577514 336975 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577515 336975 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 336975 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 336975 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
2726 1895 54 None None None Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None None None Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None None None Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None None None Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None None None Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL3349030 486807 0 None None None Human 7.1 pIC50 = 7.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
168295644 375345 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 375345 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL227833 485298 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1009 14 10 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
24774358 310913 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL400866 310913 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL188459 484959 0 None None None Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL191120 484981 0 None None None Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.2 CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
122184910 241128 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 241128 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408286 277945 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 277945 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
9958649 252383 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 252383 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
137641398 314192 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 314192 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11753695 22707 5 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 22707 5 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
44397410 252385 0 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363740 252385 0 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
52918026 123572 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 123572 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3349030 486807 0 None None None Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
137658158 315551 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 315551 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44431513 292523 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391704 292523 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
44445082 310359 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 310359 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600921 487206 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5087839 479291 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1864 23 22 21 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
127053936 298873 0 None None None Human 8.1 pIC50 = 8.1 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3968918 298873 0 None None None Human 8.1 pIC50 = 8.1 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3600842 487201 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
168285801 374542 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 374542 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
44347838 196977 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL263585 196977 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
44396986 139715 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 139715 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 139715 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 139715 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
10188529 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL365401 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
176 823 54 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
122184577 241003 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 241003 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1212 3415 38 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 3415 38 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 3415 38 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 3415 38 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 3415 38 None None None Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44348183 197480 0 None None None Human 4.0 pIC50 = 4.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL268094 197480 0 None None None Human 4.0 pIC50 = 4.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44396986 139715 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 139715 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 139715 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 139715 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL442504 484358 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL415165 488387 0 None -1 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 2006 60 27 28 -7.9 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)C(C)C 10.1021/jm0501432
CHEMBL414718 488362 0 None -2 4 Human 9.6 pKi = 9.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1846 55 24 24 -5.9 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
CHEMBL408843 488035 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1125 15 14 14 -1.6 CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
57646411 158565 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 158565 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
122194229 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
1324 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
16197727 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
4836 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL3629347 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL441738 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
DB04931 621 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL1923667 484989 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1562 47 22 18 -2.0 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm201226w
CHEMBL1923665 484988 0 None -1 3 Human 9.1 pKi = 9.1 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1601 47 23 18 -1.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm201226w
CHEMBL266879 486215 0 None -3 4 Human 9.1 pKi = 9.1 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1322 40 18 16 -2.9 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0501432
CHEMBL2370964 485647 0 None -1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1601 47 21 18 -1.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
57646437 158566 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684621 158566 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929804 158566 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070246 158566 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
56851058 141336 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57394091 141336 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
91930626 141336 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
CHEMBL1923666 141336 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57646441 158564 0 None -13 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 158564 0 None -13 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57817773 158569 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684623 158569 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929806 158569 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070249 158569 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
172445058 387891 0 None -158 3 Mouse 6.0 pKi = 6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5405613 387891 0 None -158 3 Mouse 6.0 pKi = 6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
9915636 139111 0 None -48 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186083 139111 0 None -48 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44395681 139157 0 None -70 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186289 139157 0 None -70 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
16046215 161548 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
CHEMBL213122 161548 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
16046215 161548 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
CHEMBL213122 161548 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
9915636 139111 0 None -48 4 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL186083 139111 0 None -48 4 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
156010247 351026 0 None -5 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
CHEMBL4633001 351026 0 None -5 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
44434706 180426 0 None -7 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237504 180426 0 None -7 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434860 180870 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238159 180870 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44434632 293019 0 None -1 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392096 293019 0 None -1 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434601 293179 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL392223 293179 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434870 294836 0 None -4 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL393553 294836 0 None -4 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
71454518 160640 0 None -6 4 Human 5.0 pKi = 5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL2113315 160640 0 None -6 4 Human 5.0 pKi = 5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
2817655 470403 2 None None None Human 4.0 pKi = 4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 297 4 1 1 5.3 c1ccc2cc(CNCc3cccc4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8129 470403 2 None None None Human 4.0 pKi = 4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 297 4 1 1 5.3 c1ccc2cc(CNCc3cccc4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
11191792 139471 0 None None None Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 4.7 CC1C(=O)NCCN1/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL187757 139471 0 None None None Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 4.7 CC1C(=O)NCCN1/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
9958649 252383 0 None 53 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 252383 0 None 53 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL2070373 477531 0 None -14 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2004 60 24 26 -1.2 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577062 385891 0 None -26 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL525177 385891 0 None -26 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44577090 352577 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467771 352577 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44577060 371273 0 None -316 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 371273 0 None -316 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434692 179383 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235176 179383 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434841 179560 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 455 11 4 2 4.9 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236022 179560 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 455 11 4 2 4.9 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10137615 180565 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237692 180565 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434754 181062 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 181062 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434862 181073 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238368 181073 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44434600 295284 0 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393918 295284 0 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434763 297990 0 None -17 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL396111 297990 0 None -17 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
6918276 39502 6 None -12 8 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 39502 6 None -12 8 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
168282596 373981 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL5185132 373981 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL2370966 485649 0 None 28 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1525 47 20 18 -3.0 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
9808720 136553 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
9960253 136553 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL180892 136553 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 136553 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
24848995 236780 0 None -50 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 236780 0 None -50 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44415417 161605 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL213380 161605 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
23635235 331318 0 None -223 5 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 331318 0 None -223 5 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
10232787 277668 0 None -165 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380855 277668 0 None -165 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
24740419 294881 0 None -478 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
CHEMBL393584 294881 0 None -478 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
44397281 254515 0 None -109 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365237 254515 0 None -109 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434694 179460 0 None -5 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235589 179460 0 None -5 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44434611 179473 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL235627 179473 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44435220 180103 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236803 180103 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434701 180332 0 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL237291 180332 0 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
10177247 180344 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237314 180344 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434599 180747 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 333 7 2 2 3.7 NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237957 180747 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 333 7 2 2 3.7 NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434581 331854 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL428903 331854 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
71461662 160606 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2113280 160606 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2070374 477532 2 None -22 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2091 63 26 29 -4.9 CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577092 352556 0 None -11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467586 352556 0 None -11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44347119 233438 0 None -346 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 233438 0 None -346 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44433294 309191 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL397580 309191 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
164610096 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
164620129 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456626 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4852476 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4866219 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5419394 368170 0 None -72 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456058 388500 0 None -81 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5417913 388500 0 None -81 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/acs.jmedchem.3c00432
23653113 179511 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235798 179511 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434616 179554 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236003 179554 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434570 180608 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237719 180608 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434598 180645 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237743 180645 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168289584 374841 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5198158 374841 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL2370968 485651 0 None -70 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1561 44 19 17 -1.4 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44347331 40216 0 None -257 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None -257 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44323234 40519 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347221 40519 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL124169 40519 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 40519 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11226756 238670 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 238670 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
10211466 333537 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL438432 333537 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44397283 139452 0 None -112 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL187659 139452 0 None -112 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44393418 311635 0 None -14 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL405150 311635 0 None -14 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
2852098 470306 11 None 1 3 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8045 470306 11 None 1 3 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
11272524 139150 0 None None None Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 6 2 2 6.9 CC1CC(C)CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186249 139150 0 None None None Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 6 2 2 6.9 CC1CC(C)CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
57817730 158567 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684622 158567 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929805 158567 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070247 158567 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL438235 488705 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1668 35 21 20 -1.9 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44323234 40519 0 None -16 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347221 40519 0 None -16 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 40519 0 None -16 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432377 40519 0 None -16 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL214332 485136 29 None -100 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
44265672 24480 0 None -6 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159699 24480 0 None -6 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44265707 24483 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159701 24483 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434790 181065 0 None 1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238353 181065 0 None 1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434703 292819 0 None -12 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL391944 292819 0 None -12 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434765 317297 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL413982 317297 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
51346771 121016 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL1682208 121016 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL2370553 477661 0 None -10 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1520 26 17 20 -2.1 CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
44400935 143094 0 None -104 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
CHEMBL195110 143094 0 None -104 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
164613676 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
164619641 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172451922 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172463893 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4861645 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4865888 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5406385 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5435335 368738 1 None -14 3 Mouse 5.8 pKi = 5.8 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
44432966 293011 0 None -1659 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL392092 293011 0 None -1659 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44393417 196927 0 None -40 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL263182 196927 0 None -40 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434865 179608 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL236226 179608 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
10200110 180562 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237687 180562 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434828 294810 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393532 294810 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434702 296193 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL394646 296193 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
2044 331721 54 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 331721 54 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 331721 54 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
DB01229 331721 54 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL2370963 485646 0 None -11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1562 47 20 18 -2.4 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
10408 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
5329 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
CHEMBL2070241 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
DB11653 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
16007285 162566 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL215659 162566 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL409049 488045 0 None -141 3 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1555 30 20 19 -2.5 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44434855 180858 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
11375529 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44393441 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL185195 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL351400 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44392514 251924 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362670 251924 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434794 179378 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235147 179378 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434850 180031 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236645 180031 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434656 180851 0 None -6 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 401 10 2 2 5.2 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238136 180851 0 None -6 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 401 10 2 2 5.2 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11284919 138483 0 None None None Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 605 7 2 3 7.3 Cc1ccc(C)c(N2CCN(/C(=N/c3ccc(C(=O)NCCc4ccc(Cl)cc4Cl)cc3)NC3CCCCC3)CC2)c1 10.1021/jm0400496
CHEMBL184385 138483 0 None None None Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 605 7 2 3 7.3 Cc1ccc(C)c(N2CCN(/C(=N/c3ccc(C(=O)NCCc4ccc(Cl)cc4Cl)cc3)NC3CCCCC3)CC2)c1 10.1021/jm0400496
CHEMBL420167 488424 0 None -11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 918 11 12 10 -0.9 NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
11341045 138459 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 138459 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
23635107 182366 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
CHEMBL240571 182366 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
23635107 182366 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240571 182366 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44562440 352942 0 None -27 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL471340 352942 0 None -27 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
44392535 136603 0 None -33 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL180937 136603 0 None -33 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434872 179423 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235382 179423 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434758 179553 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL236002 179553 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
9924916 179867 0 None 2 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236447 179867 0 None 2 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434781 180732 0 None -23 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 180732 0 None -23 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
9969456 294313 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393125 294313 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434863 294832 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393552 294832 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
2163781 197684 7 None 1 3 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269653 197684 7 None 1 3 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
168281969 374344 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 374344 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL1201469 38416 0 None -1 4 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL438030 488691 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1551 47 21 18 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44397304 254793 0 None -158 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365465 254793 0 None -158 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
10270570 179891 0 None -4 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236450 179891 0 None -4 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434639 294844 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393557 294844 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168273045 373348 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5175392 373348 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168281969 374344 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 374344 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
11375764 138978 0 None 398 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 138978 0 None 398 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
59149264 158448 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 158448 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 158448 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 158448 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL331259 486767 0 None -70 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 936 15 11 9 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
172443052 387786 0 None -125 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 785 18 9 7 0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5403689 387786 0 None -125 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 785 18 9 7 0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172449584 388013 0 None -154 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5408661 388013 0 None -154 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 855 21 11 7 0.6 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172440979 387523 0 None -100 3 Mouse 5.7 pKi = 5.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 814 19 9 7 0.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5397924 387523 0 None -100 3 Mouse 5.7 pKi = 5.7 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 814 19 9 7 0.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.3c00432
44410802 277672 0 None -114 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380858 277672 0 None -114 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
44434661 179371 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL235136 179371 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
44434683 180147 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL236847 180147 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
9946358 298594 0 None 1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCN(CCCc1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396655 298594 0 None 1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCN(CCCc1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434635 333526 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438334 333526 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11364326 138975 0 None 27 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 138975 0 None 27 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL410168 488101 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1527 30 20 19 -3.3 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL427629 488478 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL437050 484343 3 None -3 3 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1570 47 21 19 -2.9 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm030119t
16038315 276113 0 None -309 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
CHEMBL378046 276113 0 None -309 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
44434685 180028 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236638 180028 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434839 179512 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235802 179512 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434767 180564 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237689 180564 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434682 295286 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393919 295286 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434771 295470 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394073 295470 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
1800 473856 65 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2247 1042 63 None -46 37 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None -46 37 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None -46 37 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None -46 37 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None -46 37 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL2370533 477660 0 None -10 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1538 26 17 20 -2.0 CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL263878 486112 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
156015336 351466 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
CHEMBL4639782 351466 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
44434652 180729 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237912 180729 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434707 296228 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL394667 296228 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
10077773 178140 4 None -1122 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233135 178140 4 None -1122 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434769 180568 0 None -13 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237698 180568 0 None -13 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434857 310475 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398980 310475 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168286369 374770 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5197030 374770 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168283984 374312 0 None -3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190172 374312 0 None -3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
11785639 255417 0 None None None Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.3 NC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
CHEMBL366036 255417 0 None None None Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.3 NC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
44400812 143530 0 None -457 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 667 12 3 5 6.3 O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195734 143530 0 None -457 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 667 12 3 5 6.3 O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11156852 137980 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL183434 137980 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
11156852 137980 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
CHEMBL183434 137980 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
44434592 180345 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237315 180345 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434753 180563 0 None -9 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 699 12 3 4 9.1 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
CHEMBL237688 180563 0 None -9 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 699 12 3 4 9.1 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
10159196 180567 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237694 180567 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10269187 180944 0 None -4 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.5 NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL238180 180944 0 None -4 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.5 NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434868 296232 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL394669 296232 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL407809 487986 0 None -851 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1356 25 18 17 -2.8 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL433645 488592 0 None -6 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 -0.4 NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL428326 488513 0 None -47 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1958 57 25 26 -6.9 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
24873537 289751 0 None -20 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 289751 0 None -20 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
11181804 256447 0 None -21 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 256447 0 None -21 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44434562 179557 0 None -301 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236014 179557 0 None -301 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
44347378 233448 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333262 233448 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434843 179559 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 179559 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434657 181061 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434658 181061 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 181061 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 181061 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
1016 8173 46 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL6067481 479736 0 None -1 3 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
168271899 373686 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5180727 373686 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
164613676 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
164619641 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172451922 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172463893 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4861645 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4865888 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5406385 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5435335 368738 1 None -14 3 Mouse 6.6 pKi = 6.6 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
44433264 180191 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236940 180191 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44347379 233449 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333263 233449 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44265496 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
9968756 180340 0 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237299 180340 0 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
10292084 295077 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL393755 295077 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434614 298226 1 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396341 298226 1 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265496 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL267020 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL266417 484238 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
44322868 215692 0 None -4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 215692 0 None -4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11341046 139167 0 None 57 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 139167 0 None 57 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
44394079 254735 0 None -9 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL365278 254735 0 None -9 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
71461657 160529 0 None 4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113144 160529 0 None 4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44434845 294595 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393350 294595 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
2750 64617 55 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
6604850 64617 55 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL1398683 64617 55 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 64617 55 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
DB09201 64617 55 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL439128 488768 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
10033237 141334 0 None -158 4 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
44322896 141334 0 None -158 4 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
CHEMBL1923662 141334 0 None -158 4 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
CHEMBL431801 141334 0 None -158 4 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
CHEMBL2070254 477530 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2023 62 26 26 -1.9 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11296600 241507 0 None -41 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 241507 0 None -41 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44347106 234049 0 None -46 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL334309 234049 0 None -46 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44265496 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 197371 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
10132207 179510 0 None -7 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 343 5 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235797 179510 0 None -7 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 343 5 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434843 179559 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 179559 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL268851 486276 0 None -33 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
168279695 374206 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 374206 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168285313 374465 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 374465 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
6918814 255024 0 None -154 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL365597 255024 0 None -154 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
58777892 160534 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
CHEMBL2113149 160534 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
44434799 179462 0 None 1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235592 179462 0 None 1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434653 292529 0 None -36 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391706 292529 0 None -36 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265347 197291 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL266305 197291 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
11192466 138381 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 577 7 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm0400496
CHEMBL183842 138381 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 577 7 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm0400496
9946241 180272 0 None -7 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237079 180272 0 None -7 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434687 315333 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410179 315333 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
70688853 158568 0 None -9 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070248 158568 0 None -9 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57817763 158571 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 158571 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 158571 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 158571 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
59149255 158572 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 158572 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 158572 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 158572 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
56851059 141337 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57390568 141337 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
91930628 141337 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
CHEMBL1923668 141337 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
168279695 374206 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 374206 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44400864 252355 0 None -177 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363576 252355 0 None -177 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11410616 137574 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 579 7 2 5 5.7 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ncccn3)CC2)cc1 10.1021/jm0400496
CHEMBL182844 137574 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 579 7 2 5 5.7 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ncccn3)CC2)cc1 10.1021/jm0400496
44322869 215840 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 215840 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44434603 180741 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237935 180741 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434686 293308 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL392316 293308 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
23635237 182263 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
CHEMBL240364 182263 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
23635237 182263 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL240364 182263 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
44434688 180030 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236640 180030 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434690 180150 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434587 180277 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237094 180277 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434849 293552 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL392521 293552 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
168295173 375344 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 375344 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44562414 350776 0 None -13 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL460942 350776 0 None -13 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL2370965 485648 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1586 47 19 17 -0.7 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44434597 180442 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237530 180442 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44577093 352557 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467587 352557 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
23635235 331318 0 None -223 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
CHEMBL427860 331318 0 None -223 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
23635236 182406 0 None -60 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240780 182406 0 None -60 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434584 298579 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL396638 298579 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
10180932 180247 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237051 180247 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434657 181061 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434658 181061 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 181061 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 181061 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
10225762 292531 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL391707 292531 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
2683 202943 22 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 202943 22 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
DB11073 202943 22 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
44400934 142856 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194987 142856 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44400813 143317 0 None -120 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195308 143317 0 None -120 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11785893 139307 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 530 6 2 3 6.0 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)O1 10.1021/jm0400496
CHEMBL187022 139307 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 530 6 2 3 6.0 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)O1 10.1021/jm0400496
10108894 180566 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
CHEMBL237693 180566 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
44434621 293015 0 None -11 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL392094 293015 0 None -11 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
11477853 139182 0 None 38 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 139182 0 None 38 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
44434568 180033 0 None -81 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236650 180033 0 None -81 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
23635236 182406 0 None -60 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
CHEMBL240780 182406 0 None -60 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
11443753 139133 0 None None None Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 516 10 2 2 7.0 CCCN(CCC)/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL186189 139133 0 None None None Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 516 10 2 2 7.0 CCCN(CCC)/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
44434696 295874 0 None -36 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394394 295874 0 None -36 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265487 197689 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269689 197689 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
10025669 197698 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269776 197698 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
25444 311590 1 None None None Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL404811 311590 1 None None None Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL412523 488229 0 None -125 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1388 25 18 17 -1.7 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
8447 372118 60 None -50 13 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 372118 60 None -50 13 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
DB14201 372118 60 None -50 13 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
44265711 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44265749 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434847 179815 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236442 179815 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434864 181074 0 None -13 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238369 181074 0 None -13 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
3198 461850 54 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44433439 180752 0 None -44 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL237976 180752 0 None -44 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44434684 293307 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392315 293307 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265312 470492 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 286 4 2 1 4.6 c1ccc2c(CNCc3c[nH]c4ccccc34)cccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8208 470492 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 286 4 2 1 4.6 c1ccc2c(CNCc3c[nH]c4ccccc34)cccc2c1 10.1016/s0960-894x(02)00088-4
51346770 121017 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
CHEMBL1682209 121017 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
127036484 5482 39 None -346 4 Human 7.4 pKi = 7.4 Binding
Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
1323 5482 39 None -346 4 Human 7.4 pKi = 7.4 Binding
Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
92432 5482 39 None -346 4 Human 7.4 pKi = 7.4 Binding
Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL3735690 5482 39 None -346 4 Human 7.4 pKi = 7.4 Binding
Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL430239 5482 39 None -346 4 Human 7.4 pKi = 7.4 Binding
Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1024 17 13 11 -1.2 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
44577094 352558 0 None -117 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467588 352558 0 None -117 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434766 310744 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 310744 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44320339 470908 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL85918 470908 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
10025669 197698 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL269776 197698 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL385465 487662 0 None -44 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 960 12 12 10 -0.8 CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL2070244 485054 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1543 35 24 20 -7.2 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
59149266 158570 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693081 158570 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929807 158570 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070250 158570 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44347331 40216 0 None -257 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None -257 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
171378453 388656 0 None -251 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 799 19 9 7 0.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5421386 388656 0 None -251 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 799 19 9 7 0.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
44577063 371320 0 None -74 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL498150 371320 0 None -74 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
71458055 160518 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
CHEMBL2113133 160518 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
44434689 180032 0 None -33 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236649 180032 0 None -33 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434861 181072 0 None -9 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238367 181072 0 None -9 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168285313 374465 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 374465 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44265374 473451 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8825 473451 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL415661 488409 0 None -295 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1372 25 18 17 -2.2 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
10283036 277531 0 None -72 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380540 277531 0 None -72 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
44265711 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44265749 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 473921 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434778 180572 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
10178845 180742 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237937 180742 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434762 309160 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 309160 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44265309 470487 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8201 470487 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
2436 470362 35 None -25 14 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
68617 470362 35 None -25 14 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 470362 35 None -25 14 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
DB01104 470362 35 None -25 14 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
11433304 138958 0 None None None Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 591 8 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0400496
CHEMBL185398 138958 0 None None None Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 591 8 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0400496
44434704 180029 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236639 180029 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434780 294859 0 None -9 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 525 8 2 2 7.3 NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393568 294859 0 None -9 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 525 8 2 2 7.3 NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1 10.1016/j.bmc.2007.06.003
44265351 470579 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 8 2 3 4.7 N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8287 470579 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 8 2 3 4.7 N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
56851057 141335 0 None -190 3 Human 7.3 pKi = 7.3 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1069 34 13 10 1.3 C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1021/jm201226w
CHEMBL1923664 141335 0 None -190 3 Human 7.3 pKi = 7.3 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1069 34 13 10 1.3 C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1021/jm201226w
44434662 179372 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235137 179372 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434636 180144 0 None 1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236841 180144 0 None 1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434647 180419 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
CHEMBL237483 180419 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
44397028 252079 0 None -61 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
CHEMBL363019 252079 0 None -61 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
44434690 180150 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265472 473327 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8742 473327 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL441760 488836 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1555 30 20 19 -2.5 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC(C)(C)[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44397030 139652 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL188651 139652 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44347105 232395 0 None -43 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL331728 232395 0 None -43 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434854 180857 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 180857 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434855 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
126736894 366943 28 None -213 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC5R assessed as inhibition constantBinding affinity to human MC5R assessed as inhibition constant
ChEMBL 675 9 1 6 6.0 COC[C@H]1CN(C(=O)[C@]2(F)CN(C3CCCC3)C[C@H]2c2ccc(OC)cc2)C[C@@H]1c1ccc(C(F)(F)F)cc1N1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.4c02358
CHEMBL4802160 366943 28 None -213 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC5R assessed as inhibition constantBinding affinity to human MC5R assessed as inhibition constant
ChEMBL 675 9 1 6 6.0 COC[C@H]1CN(C(=O)[C@]2(F)CN(C3CCCC3)C[C@H]2c2ccc(OC)cc2)C[C@@H]1c1ccc(C(F)(F)F)cc1N1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.4c02358
44347081 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347082 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347330 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL420727 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432407 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL436169 328872 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434772 179456 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434690 180150 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10109225 310705 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL399624 310705 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434867 179381 0 None -22 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL235162 179381 0 None -22 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434714 295074 0 None -10 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393753 295074 0 None -10 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL2070242 485053 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1510 32 22 20 -6.9 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11237444 255419 0 None 245 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 255419 0 None 245 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
11249545 138497 0 None 61 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 138497 0 None 61 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11752660 138470 0 None None None Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 2 3 5.1 CN1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
CHEMBL184323 138470 0 None None None Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 2 3 5.1 CN1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
164610096 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
164620129 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172456626 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4852476 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL4866219 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5419394 368170 0 None -72 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.3c00432
172452729 388263 0 None -63 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 771 17 9 7 -0.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CN)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413452 388263 0 None -63 3 Mouse 6.3 pKi = 6.3 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 771 17 9 7 -0.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CN)C(N)=O 10.1021/acs.jmedchem.3c00432
16007264 161185 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL211564 161185 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
16007264 161185 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
CHEMBL211564 161185 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
44347110 233133 0 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL332762 233133 0 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
10864861 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
10886436 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
10952071 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
1338 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
9938402 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL140108 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL334457 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL339053 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL342954 8293 40 None -154 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
44434713 180425 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 180425 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434855 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44265713 473772 0 None None None Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 364 6 3 4 1.9 O=C(NCCc1c[nH]cn1)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9048 473772 0 None None None Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 364 6 3 4 1.9 O=C(NCCc1c[nH]cn1)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434663 179373 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235138 179373 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
24740655 179943 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
CHEMBL236521 179943 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
24740655 179943 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL236521 179943 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
44434760 179375 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235140 179375 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434764 179419 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235358 179419 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10157774 180145 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236842 180145 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434859 180862 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
CHEMBL238158 180862 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
168295173 375344 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 375344 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44456219 308755 0 None -112 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL403806 308755 0 None -112 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44347219 40465 0 None -1071 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 40465 0 None -1071 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
25211670 348318 0 None -56 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454916 348318 0 None -56 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
44562460 372406 0 None -165 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL511826 372406 0 None -165 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
6918850 253432 0 None -154 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
CHEMBL364560 253432 0 None -154 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
44434690 180150 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434654 180849 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238134 180849 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434664 179417 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434665 179417 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235355 179417 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393383 179417 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434772 179456 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434778 180572 0 None -10 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -10 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434595 295551 0 None -7 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 419 9 2 3 5.6 CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL394149 295551 0 None -7 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 419 9 2 3 5.6 CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
6918844 333287 0 None -173 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
CHEMBL436122 333287 0 None -173 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
11179871 252259 0 None None None Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 4.5 O=C1CN(/C(=N\C2CCCCC2)Nc2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)CCN1 10.1021/jm0400496
CHEMBL363440 252259 0 None None None Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 4.5 O=C1CN(/C(=N\C2CCCCC2)Nc2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)CCN1 10.1021/jm0400496
44434855 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44265589 336570 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44265591 336570 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL447178 336570 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL8720 336570 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44434634 180143 0 None -31 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236840 180143 0 None -31 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
44323020 333622 0 None -741 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 333622 0 None -741 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL1923663 484987 0 None -31 3 Human 7.2 pKi = 7.2 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 846 23 11 8 0.7 CC(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
10134057 179516 0 None -32 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235815 179516 0 None -32 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11786860 138626 1 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185035 138626 1 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44432964 178325 0 None -1513 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233372 178325 0 None -1513 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL2370154 477645 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 1038 17 14 11 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
11215758 138373 0 None -125 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptorBinding affinity for human melanocortin 5 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL183799 138373 0 None -125 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptorBinding affinity for human melanocortin 5 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
24180592 197336 0 None -177 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 197336 0 None -177 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44265708 331631 0 None -1 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44265719 331631 0 None -1 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL428480 331631 0 None -1 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL9219 331631 0 None -1 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL11359 24083 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
44434821 180856 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238149 180856 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL427666 488485 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 1368 41 18 17 -2.6 CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O 10.1021/jm0501432
172447220 387427 0 None None None Mouse 7.2 pKi = 7.2 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase assessed as inhibition constantBinding affinity to mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase assessed as inhibition constant
ChEMBL 1099 17 12 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cn(C)cn2)NC1=O 10.1021/acs.jmedchem.3c00432
CHEMBL5396011 387427 0 None None None Mouse 7.2 pKi = 7.2 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase assessed as inhibition constantBinding affinity to mouse MC5R expressed in HEK293 cells coexpressing CRE/beta-galactosidase assessed as inhibition constant
ChEMBL 1099 17 12 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cn(C)cn2)NC1=O 10.1021/acs.jmedchem.3c00432
44434848 179826 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL236443 179826 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44347840 317432 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
91932630 317432 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL415333 317432 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44347220 333129 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 333129 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434766 310744 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 310744 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44322795 473859 0 None -114 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 473859 0 None -114 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44265715 24484 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159702 24484 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434856 310442 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398777 310442 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44577091 352578 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467772 352578 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434778 180572 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434651 180728 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237911 180728 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434698 335567 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL445669 335567 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44400863 141426 0 None -151 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192464 141426 0 None -151 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434855 180858 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434785 295471 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394074 295471 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
11295934 139263 0 None None None Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 558 8 3 2 7.1 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\Cc2cc(F)cc(F)c2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186792 139263 0 None None None Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 558 8 3 2 7.1 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\Cc2cc(F)cc(F)c2)NC2CCCCC2)cc1 10.1021/jm0400496
10325955 330164 0 None -6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 330164 0 None -6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
71452732 160524 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113139 160524 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44347081 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347082 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347330 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL420727 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432407 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL436169 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
70693083 158573 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929813 158573 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070253 158573 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
24740653 179451 0 None -190 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL235556 179451 0 None -190 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
2726 1895 54 None -95 48 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None -95 48 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None -95 48 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None -95 48 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None -95 48 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL407213 487949 0 None -169 3 Human 6.1 pKi = 6.1 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 823 10 10 8 -0.2 CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
11180881 139108 1 None -47 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
CHEMBL186074 139108 1 None -47 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
44434695 180266 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237070 180266 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434768 310745 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL399811 310745 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44400660 142962 0 None -301 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195071 142962 0 None -301 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44396002 252795 0 None -17 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
CHEMBL364215 252795 0 None -17 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
10158674 294607 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393359 294607 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265589 336570 0 None -2 3 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44265591 336570 0 None -2 3 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL447178 336570 0 None -2 3 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL8720 336570 0 None -2 3 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44265479 470876 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 268 2 2 2 1.9 N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(02)00088-4
CHEMBL8561 470876 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 268 2 2 2 1.9 N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(02)00088-4
44434713 180425 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 180425 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL412536 488230 18 None -87 4 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 2659 85 36 37 -10.0 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)O 10.1021/jm0501432
44434754 181062 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 181062 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
11365127 252133 0 None None None Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 569 7 2 3 6.6 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCC(N3CCCC3)CC2)cc1 10.1021/jm0400496
CHEMBL363290 252133 0 None None None Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 569 7 2 3 6.6 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCC(N3CCCC3)CC2)cc1 10.1021/jm0400496
44434782 180855 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238144 180855 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434772 179456 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434637 180252 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237052 180252 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL409636 488073 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 1604 35 21 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
44456222 198224 0 None -676 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 198224 0 None -676 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
172449408 388260 0 None -100 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172449794 388260 0 None -100 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413381 388260 0 None -100 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5414015 388260 0 None -100 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.3c00432
172449003 388268 0 None -245 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 842 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(N)=O)C(N)=O 10.1021/acs.jmedchem.3c00432
CHEMBL5413535 388268 0 None -245 3 Mouse 6.1 pKi = 6.1 Binding
Binding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysisBinding affinity to mouse MC5R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
ChEMBL 842 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(N)=O)C(N)=O 10.1021/acs.jmedchem.3c00432
44434666 179418 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235356 179418 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
44434650 180727 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237910 180727 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434648 294846 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393558 294846 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44393421 241661 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL361052 241661 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434797 179461 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235590 179461 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434691 180265 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL237069 180265 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434770 179420 0 None -46 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235359 179420 0 None -46 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265473 473328 0 None -9 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 200 4 2 2 1.9 NCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8743 473328 0 None -9 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 200 4 2 2 1.9 NCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
172461915 389107 0 None -1819 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells measured for 2 hrs by microbeta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells measured for 2 hrs by microbeta counter analysis
ChEMBL 464 4 1 8 3.0 COc1cc([C@@H](C)C(=O)N2CC[C@@]3(COc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1 10.1021/acs.jmedchem.2c02012
CHEMBL5432266 389107 0 None -1819 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells measured for 2 hrs by microbeta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells measured for 2 hrs by microbeta counter analysis
ChEMBL 464 4 1 8 3.0 COc1cc([C@@H](C)C(=O)N2CC[C@@]3(COc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1 10.1021/acs.jmedchem.2c02012
44434690 180733 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237920 180733 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
24180646 294869 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 294869 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
24180646 294869 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 294869 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
44434633 180027 0 None -35 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236630 180027 0 None -35 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434699 180331 0 None -26 3 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 531 10 2 3 7.7 CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237290 180331 0 None -26 3 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 531 10 2 3 7.7 CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
24741624 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
44416197 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
44416349 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL215617 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL377231 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL425261 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
24741624 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44416197 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44416349 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL215617 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL377231 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL425261 162554 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
10864861 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
10886436 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
10952071 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
1338 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
9938402 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL140108 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL334457 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL339053 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL342954 8293 40 None -154 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
44265639 24478 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159697 24478 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
44434884 179470 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235617 179470 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434690 180150 0 None -8 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -8 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434655 180850 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238135 180850 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10260053 332923 0 None -6 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 332923 0 None -6 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
44432932 178618 0 None -263 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233758 178618 0 None -263 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434700 296189 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 637 12 3 4 9.0 CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL394645 296189 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 637 12 3 4 9.0 CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434762 309160 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 309160 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
10155513 298185 0 None -9 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396303 298185 0 None -9 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
176 823 54 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
1212 3415 38 None -114 41 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 3415 38 None -114 41 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 3415 38 None -114 41 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 3415 38 None -114 41 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 3415 38 None -114 41 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
122194229 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
1324 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
16197727 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
4836 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
CHEMBL3629347 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
CHEMBL441738 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
DB04931 621 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201226w
11318528 138548 0 None None None Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 7 2 2 7.1 CN(/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1)C1CCCCC1 10.1021/jm0400496
CHEMBL184612 138548 0 None None None Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 7 2 2 7.1 CN(/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1)C1CCCCC1 10.1021/jm0400496
44410803 277461 0 None -87 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380365 277461 0 None -87 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44434880 179469 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235616 179469 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434709 180604 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237714 180604 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434854 180857 0 None -1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 180857 0 None -1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434787 295472 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394075 295472 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434605 296194 0 None -13 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
CHEMBL394647 296194 0 None -13 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
10304463 158422 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL206840 158422 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
44397198 139052 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL185862 139052 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
10291370 292679 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391823 292679 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434772 179456 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44393450 251729 0 None -2 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362010 251729 0 None -2 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44562287 348306 0 None -102 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454900 348306 0 None -102 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
6918857 276064 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL377961 276064 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
44434693 332134 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL429451 332134 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44265708 331631 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44265719 331631 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL428480 331631 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL9219 331631 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44434697 295373 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL393994 295373 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434759 179374 0 None -23 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235139 179374 0 None -23 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
25058412 372568 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL513404 372568 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434851 180737 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237930 180737 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434761 180024 0 None -14 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236626 180024 0 None -14 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10257541 254315 0 None -602 4 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL365039 254315 0 None -602 4 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
46877881 465190 0 None -5 3 Human 6.0 pKi = 6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 465190 0 None -5 3 Human 6.0 pKi = 6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11296732 290574 0 None -22 3 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL390130 290574 0 None -22 3 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
23661656 180153 0 None -181 5 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434575 180153 0 None -181 5 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236872 180153 0 None -181 5 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 180153 0 None -181 5 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
11296732 290574 0 None -22 3 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL390130 290574 0 None -22 3 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
1326 7717 0 None -12 4 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15840392
1329 645 0 None -5011 3 Mouse 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
Q03288 645 0 None -5011 3 Mouse 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
1320 757 0 None None None Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16162729 757 0 None None None Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
P01189 757 0 None None None Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
P01193 757 0 None None None Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
P01194 757 0 None None None Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1328 3975 0 None -10 4 Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9832440
127035019 7320 11 None -5 3 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
1325 7320 11 None -5 3 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
9898183 7320 11 None -5 3 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
CHEMBL3422426 7320 11 None -5 3 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
CHEMBL3735607 7320 11 None -5 3 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
3198 461850 54 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
983 461850 54 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 461850 54 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
DB01127 461850 54 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1016 8173 46 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 8173 46 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 8173 46 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 8173 46 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 8173 46 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1800 473856 65 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4189 473856 65 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 473856 65 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
DB01110 473856 65 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2044 331721 54 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
36314 331721 54 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
CHEMBL428647 331721 54 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
DB01229 331721 54 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
176 823 54 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 823 54 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 823 54 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 823 54 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 823 54 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
1212 3415 38 None -114 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 3415 38 None -114 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 3415 38 None -114 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 3415 38 None -114 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 3415 38 None -114 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2726 1895 54 None -95 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 1895 54 None -95 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 1895 54 None -95 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 1895 54 None -95 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 1895 54 None -95 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2436 470362 35 None -25 14 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
68617 470362 35 None -25 14 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 470362 35 None -25 14 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
DB01104 470362 35 None -25 14 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2247 1042 63 None -46 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 1042 63 None -46 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 1042 63 None -46 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 1042 63 None -46 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 1042 63 None -46 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
11993702 7304 0 None -24 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
5416 7304 0 None -24 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
9272 7304 0 None -24 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
DB11700 7304 0 None -24 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
10408 1486 31 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
5329 1486 31 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379 1486 31 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
CHEMBL2070241 1486 31 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
DB11653 1486 31 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
10408 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
5329 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
9941379 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
CHEMBL2070241 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
DB11653 1486 31 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
11993702 7304 0 None -24 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
5416 7304 0 None -24 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
9272 7304 0 None -24 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
DB11700 7304 0 None -24 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
134611880 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
16132265 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
3633 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
4931 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
CHEMBL1201610 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
DB01285 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
P01189 570 0 None -2187 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675