Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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1324 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
16154396 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
16197727 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
16197727.0 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
44285019 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
57514683 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
91898441 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
DB04931 302 None 19 Mouse Functional pEC50 = 10.5 10.5 -5 8
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 None None None None 10.1021/jm101425m
CHEMBL2371966 212622 None 0 Human Functional pEC50 = 10.5 10.5 616 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
118722937 116302 None 0 Mouse Functional pEC50 = 10.4 10.4 1 3
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 116302 None 0 Mouse Functional pEC50 = 10.4 10.4 1 3
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 116306 None 0 Mouse Functional pEC50 = 10.4 10.4 1 3
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 116306 None 0 Mouse Functional pEC50 = 10.4 10.4 1 3
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 116299 None 0 Mouse Functional pEC50 = 10.3 10.3 1 3
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 116299 None 0 Mouse Functional pEC50 = 10.3 10.3 1 3
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
1324 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
16154396 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
16197727 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
16197727.0 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
44285019 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
57514683 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
91898441 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
DB04931 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
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 None None None None 10.1021/jm0492756
1324 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
16154396 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
16197727 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
16197727.0 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
44285019 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
57514683 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
91898441 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
DB04931 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
118722944 116309 None 0 Mouse Functional pEC50 = 10.2 10.2 -1 3
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 116309 None 0 Mouse Functional pEC50 = 10.2 10.2 -1 3
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
1324 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
16154396 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
16197727 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
16197727.0 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
44285019 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
57514683 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
91898441 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
DB04931 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
1324 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727.0 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 302 None 19 Mouse Functional pEC50 = 10.2 10.2 -5 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL414965 215626 None 0 Mouse Functional pEC50 = 10.1 10.1 -1 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1324 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16154396 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727.0 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
44285019 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
57514683 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
91898441 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
DB04931 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
1324 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
16154396 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727.0 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
44285019 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
57514683 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
91898441 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
DB04931 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
1324 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
16154396 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
16197727 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
16197727.0 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
44285019 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
57514683 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
91898441 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
DB04931 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
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 None None None None 10.1021/acsmedchemlett.0c00561
118722930 116297 None 0 Mouse Functional pEC50 = 10.1 10.1 1 3
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 116297 None 0 Mouse Functional pEC50 = 10.1 10.1 1 3
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
1324 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727.0 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 302 None 19 Mouse Functional pEC50 = 10.1 10.1 -5 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL405087 215001 None 0 Mouse Functional pEC50 = 10 10.0 -1 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1324 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16154396 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727.0 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
44285019 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
57514683 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
91898441 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
DB04931 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
1324 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
16154396 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
16197727 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
16197727.0 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
44285019 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
57514683 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
91898441 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
DB04931 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -5 8
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 None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL406842 215084 None 0 Mouse Functional pEC50 = 10.0 10.0 3 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL413212 215515 None 0 Mouse Functional pEC50 = 9.9 9.9 -6 4
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
127036484 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
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 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
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 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL410404 215279 None 0 Mouse Functional pEC50 = 9.9 9.9 11 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
118722926 116294 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
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 116294 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
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 116298 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
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 116298 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
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 116303 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
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 116303 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
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
1324 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
16154396 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
16197727 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
16197727.0 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
44285019 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
57514683 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
91898441 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
DB04931 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00860
127036484 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
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 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
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 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
1324 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
16154396 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
16197727 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
16197727.0 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
44285019 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
57514683 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
91898441 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
DB04931 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00684
CHEMBL411400 215343 None 0 Mouse Functional pEC50 = 9.9 9.9 48 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O 10.1021/jm030452x
118722942 116307 None 0 Mouse Functional pEC50 = 9.8 9.8 -1 3
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 116307 None 0 Mouse Functional pEC50 = 9.8 9.8 -1 3
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 116308 None 0 Mouse Functional pEC50 = 9.8 9.8 -1 3
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 116308 None 0 Mouse Functional pEC50 = 9.8 9.8 -1 3
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
1323 2688 None 38 Mouse Functional pEC50 = 9.8 9.8 -5 7
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
92432 2688 None 38 Mouse Functional pEC50 = 9.8 9.8 -5 7
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 9.8 9.8 -5 7
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
44310104 81619 None 0 Mouse Functional pEC50 = 9.8 9.8 -7 3
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 81619 None 0 Mouse Functional pEC50 = 9.8 9.8 -7 3
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 212598 None 0 Mouse Functional pEC50 = 9.8 9.8 -3 3
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0490843
CHEMBL405335 215016 None 0 Mouse Functional pEC50 = 9.8 9.8 2 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
118722927 116295 None 0 Mouse Functional pEC50 = 9.7 9.7 1 3
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 116295 None 0 Mouse Functional pEC50 = 9.7 9.7 1 3
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 124050 None 0 Mouse Functional pEC50 = 9.7 9.7 -7 4
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 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.10.095
CHEMBL3629347 124050 None 0 Mouse Functional pEC50 = 9.7 9.7 -7 4
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 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.10.095
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00301
1323 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm0492756
92432 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm0492756
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm0492756
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.7b00856
1323 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm501027w
92432 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm501027w
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 9.7 9.7 -5 7
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 None None None None 10.1021/jm501027w
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.3c00432
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -5 8
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 None None None None 10.1021/acs.jmedchem.1c01417
16132144 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
16133793 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
44273719 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
16132144 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
16133793 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
44273719 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.7 9.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
CHEMBL408843 215195 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 None None None CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
118722932 115582 None 0 Mouse Functional pEC50 = 9.6 9.6 1 3
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 115582 None 0 Mouse Functional pEC50 = 9.6 9.6 1 3
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 212625 None 0 Human Functional pEC50 = 9.6 9.6 1000 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0614275
1324 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 19 Human Functional pEC50 = 9.6 9.6 -13 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
1324 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
16154396 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
16197727 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
16197727.0 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
44285019 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
57514683 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
91898441 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
DB04931 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm800291b
1324 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
16154396 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
16197727 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
16197727.0 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
44285019 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
57514683 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
91898441 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
DB04931 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm500064t
122194229 124050 None 0 Mouse Functional pEC50 = 9.6 9.6 -7 4
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 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL3629347 124050 None 0 Mouse Functional pEC50 = 9.6 9.6 -7 4
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 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
1324 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
16154396 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
16197727 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
16197727.0 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
44285019 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
57514683 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
91898441 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
DB04931 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -5 8
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 None None None None 10.1021/jm301253y
CHEMBL2371971 212627 None 0 Human Functional pEC50 = 9.5 9.5 1288 2
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O 10.1021/jm0614275
CHEMBL501592 216629 None 0 Human Functional pEC50 = 9.5 9.5 37 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
134463477 159345 None 0 Mouse Functional pEC50 = 9.5 9.5 3 3
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 159345 None 0 Mouse Functional pEC50 = 9.5 9.5 3 3
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
1324 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
16154396 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
16197727 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
16197727.0 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
44285019 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
57514683 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
91898441 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
DB04931 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acsmedchemlett.9b00198
1324 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
16154396 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
16197727 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
16197727.0 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
44285019 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
57514683 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
91898441 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
DB04931 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -5 8
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 None None None None 10.1021/acs.jmedchem.5b01894
45487403 199891 None 0 Mouse Functional pEC50 = 9.5 9.5 -33 4
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 199891 None 0 Mouse Functional pEC50 = 9.5 9.5 -33 4
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 116301 None 0 Mouse Functional pEC50 = 9.5 9.5 -3 3
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 116301 None 0 Mouse Functional pEC50 = 9.5 9.5 -3 3
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 212618 None 0 Human Functional pEC50 = 9.4 9.4 8 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
CHEMBL267794 213192 None 0 Mouse Functional pEC50 = 9.4 9.4 -11 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
1324 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 19 Human Functional pEC50 = 9.4 9.4 -13 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16132144 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2003.08.078
16133793 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2003.08.078
44273719 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2003.08.078
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2003.08.078
1324 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -5 8
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 None None None None 10.1021/acs.jmedchem.8b00251
16132144 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
16133793 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
44273719 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
CHEMBL307457 213440 None 0 Mouse Functional pEC50 = 9.4 9.4 10 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL266417 213142 None 0 Mouse Functional pEC50 = 9.4 9.4 -12 6
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
16132144 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010524p
16133793 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010524p
44273719 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010524p
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010524p
16132144 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303608
16133793 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303608
44273719 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303608
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.4 9.4 -1 8
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303608
CHEMBL2371967 212623 None 0 Human Functional pEC50 = 9.4 9.4 275 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
134466953 156750 None 0 Mouse Functional pEC50 = 9.4 9.4 -1 3
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 156750 None 0 Mouse Functional pEC50 = 9.4 9.4 -1 3
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
90643803 111806 None 0 Mouse Functional pEC50 = 9.4 9.4 1 4
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 111806 None 0 Mouse Functional pEC50 = 9.4 9.4 1 4
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 214835 None 0 Mouse Functional pEC50 = 9.3 9.3 -25 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010061n
CHEMBL429236 215977 None 0 Mouse Functional pEC50 = 9.3 9.3 -21 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
10886436 119221 None 0 Mouse Functional pEC50 = 9.3 9.3 1 4
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(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
CHEMBL342954 119221 None 0 Mouse Functional pEC50 = 9.3 9.3 1 4
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(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
16132144 211738 None 29 Mouse Functional pEC50 = 9.3 9.3 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
16133793 211738 None 29 Mouse Functional pEC50 = 9.3 9.3 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
44273719 211738 None 29 Mouse Functional pEC50 = 9.3 9.3 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.3 9.3 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL410763 215298 None 0 Mouse Functional pEC50 = 9.3 9.3 -14 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL2369484 212086 None 0 Mouse Functional pEC50 = 9.3 9.3 -2 3
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL411378 215341 None 0 Mouse Functional pEC50 = 9.3 9.3 16 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1 10.1021/jm030452x
44310344 97382 None 0 Mouse Functional pEC50 = 9.3 9.3 -3 3
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 97382 None 0 Mouse Functional pEC50 = 9.3 9.3 -3 3
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 97382 None 0 Mouse Functional pEC50 = 9.3 9.3 -3 3
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 68041 None 0 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 68041 None 0 Mouse Functional pEC50 = 9.2 9.2 -1 3
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
1324 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
16154396 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
16197727 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
16197727.0 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
44285019 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
57514683 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
91898441 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
DB04931 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960845e
1324 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
16154396 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
16197727 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
16197727.0 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
44285019 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
57514683 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
91898441 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
DB04931 302 None 19 Human Functional pEC50 = 9.2 9.2 -13 8
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 None None None None 10.1021/jm960840h
16132144 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
16133793 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
44273719 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
CHEMBL264536 213086 None 9 Mouse Functional pEC50 = 9.2 9.2 -13 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm010061n
90643806 111809 None 0 Mouse Functional pEC50 = 9.2 9.2 6 4
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 111809 None 0 Mouse Functional pEC50 = 9.2 9.2 6 4
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 215933 None 0 Mouse Functional pEC50 = 9.2 9.2 -12 5
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
101670969 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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 168999 None 21 Mouse Functional pEC50 = 9.2 9.2 -1 3
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
16132144 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
16133793 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
44273719 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.2 9.2 -1 8
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
122184910 122621 None 0 Human Functional pEC50 = 9.1 9.1 2 4
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 122621 None 0 Human Functional pEC50 = 9.1 9.1 2 4
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
16132144 211738 None 29 Mouse Functional pEC50 = 9.1 9.1 -1 8
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
16133793 211738 None 29 Mouse Functional pEC50 = 9.1 9.1 -1 8
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
44273719 211738 None 29 Mouse Functional pEC50 = 9.1 9.1 -1 8
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.1 9.1 -1 8
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
90643802 111805 None 0 Mouse Functional pEC50 = 9.1 9.1 2 4
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 111805 None 0 Mouse Functional pEC50 = 9.1 9.1 2 4
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 71143 None 0 Mouse Functional pEC50 = 9.1 9.1 -2 3
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 71143 None 0 Mouse Functional pEC50 = 9.1 9.1 -2 3
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 156071 None 0 Human Functional pEC50 = 9.0 9.0 -2 3
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 156071 None 0 Human Functional pEC50 = 9.0 9.0 -2 3
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 212624 None 0 Human Functional pEC50 = 9 9.0 - 1
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL2371970 212626 None 0 Human Functional pEC50 = 9 9.0 - 1
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C2CCCCC2)NC1=O 10.1021/jm0614275
90643808 111810 None 0 Mouse Functional pEC50 = 9 9.0 7 4
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 111810 None 0 Mouse Functional pEC50 = 9 9.0 7 4
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
1324 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
16154396 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
16197727 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
16197727.0 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
44285019 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
57514683 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
91898441 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
DB04931 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
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 None None None None 10.1021/jm049579s
1324 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 19 Human Functional pEC50 = 9 9.0 -13 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
1324 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
16154396 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
16197727 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
16197727.0 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
44285019 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
57514683 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
91898441 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
DB04931 302 None 19 Human Functional pEC50 = 9.0 9.0 -13 8
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 None None None None 10.1021/acs.jmedchem.7b00353
122184635 122500 None 0 Human Functional pEC50 = 9.0 9.0 2 4
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 122500 None 0 Human Functional pEC50 = 9.0 9.0 2 4
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 111807 None 0 Mouse Functional pEC50 = 9.0 9.0 2 4
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 111807 None 0 Mouse Functional pEC50 = 9.0 9.0 2 4
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
16132144 211738 None 29 Mouse Functional pEC50 = 9.0 9.0 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
16133793 211738 None 29 Mouse Functional pEC50 = 9.0 9.0 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
44273719 211738 None 29 Mouse Functional pEC50 = 9.0 9.0 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 9.0 9.0 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
CHEMBL2096742 211665 None 0 Human Functional pEC50 = 8.9 8.9 1 6
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm801300c
CHEMBL428615 215921 None 0 Mouse Functional pEC50 = 8.9 8.9 -70 5
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
155553683 174287 None 0 Mouse Functional pEC50 = 8.9 8.9 -4 3
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 174287 None 0 Mouse Functional pEC50 = 8.9 8.9 -4 3
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 211293 None 0 Mouse Functional pEC50 = 8.8 8.8 -8 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL491870 216565 None 0 Mouse Functional pEC50 = 8.8 8.8 -3 4
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1323 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/jm960845e
92432 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/jm960845e
CHEMBL2371963 212619 None 0 Human Functional pEC50 = 8.8 8.8 295 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL500743 216612 None 0 Human Functional pEC50 = 8.8 8.8 1 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL322610 213693 None 0 Mouse Functional pEC50 = 8.8 8.8 2 4
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
155555217 174441 None 0 Mouse Functional pEC50 = 8.8 8.8 6 3
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 174441 None 0 Mouse Functional pEC50 = 8.8 8.8 6 3
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
1323 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.8 8.8 -181 7
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 None None None None 10.1021/acs.jmedchem.1c01848
118722939 116304 None 0 Mouse Functional pEC50 = 8.8 8.8 -3 3
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 116304 None 0 Mouse Functional pEC50 = 8.8 8.8 -3 3
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 212428 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](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 116305 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 3
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 116305 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 3
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 214027 None 0 Mouse Functional pEC50 = 8.7 8.7 -7 3
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 None None None C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
145976863 163853 None 0 Human Functional pEC50 = 8.7 8.7 -1 4
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 163853 None 0 Human Functional pEC50 = 8.7 8.7 -1 4
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 216651 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL443071 216381 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
118722935 116300 None 0 Mouse Functional pEC50 = 8.7 8.7 -1 3
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 116300 None 0 Mouse Functional pEC50 = 8.7 8.7 -1 3
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
1324 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
16154396 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
16197727 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
16197727.0 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
44285019 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
57514683 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
91898441 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
DB04931 302 None 19 Mouse Functional pEC50 = 8.7 8.7 -5 8
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 None None None None 10.1021/acs.jmedchem.9b00053
11787684 70298 None 0 Mouse Functional pEC50 = 8 8.0 -3 3
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 70298 None 0 Mouse Functional pEC50 = 8 8.0 -3 3
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 214676 None 1 Human Functional pEC50 = 8 8.0 -25 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
10483153 60831 None 0 Human Functional pEC50 = 6 6.0 -87 4
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 60831 None 0 Human Functional pEC50 = 6 6.0 -87 4
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 15047 None 0 Human Functional pEC50 = 6 6.0 -40 4
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 15047 None 0 Human Functional pEC50 = 6 6.0 -40 4
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
137632948 156673 None 0 Mouse Functional pEC50 = 6 6.0 -4 2
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 156673 None 0 Mouse Functional pEC50 = 6 6.0 -4 2
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 12286 None 0 Human Functional pEC50 = 6 6.0 -19 2
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 12286 None 0 Human Functional pEC50 = 6 6.0 -19 2
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
CHEMBL2028959 12286 None 0 Human Functional pEC50 = 6 6.0 -19 2
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 215108 None 0 Human Functional pEC50 = 6 6.0 - 1
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 None None None CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
155555947 174616 None 0 Mouse Functional pEC50 = 5 5.0 -77 2
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 174616 None 0 Mouse Functional pEC50 = 5 5.0 -77 2
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 31925 None 0 Human Functional pEC50 = 6 6.0 -295 2
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 31925 None 0 Human Functional pEC50 = 6 6.0 -295 2
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 167561 None 0 Human Functional pEC50 = 7.0 7.0 -91 4
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 167561 None 0 Human Functional pEC50 = 7.0 7.0 -91 4
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
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 7.0 7.0 -8 6
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 7.0 7.0 -8 6
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
164621851 185967 None 0 Mouse Functional pEC50 = 6.0 6.0 - 1
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 185967 None 0 Mouse Functional pEC50 = 6.0 6.0 - 1
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 199781 None 0 Mouse Functional pEC50 = 5.0 5.0 -8 3
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 199781 None 0 Mouse Functional pEC50 = 5.0 5.0 -8 3
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 199473 None 0 Mouse Functional pEC50 = 5.0 5.0 -9 2
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 199473 None 0 Mouse Functional pEC50 = 5.0 5.0 -9 2
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 214274 None 0 Human Functional pEC50 = 6.0 6.0 -9 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
137633806 156572 None 0 Human Functional pEC50 = 7.0 7.0 -38 3
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 156572 None 0 Human Functional pEC50 = 7.0 7.0 -38 3
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 213067 None 0 Mouse Functional pEC50 = 8.0 8.0 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
155563055 175399 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 3
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 175399 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 3
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 213683 None 0 Mouse Functional pEC50 = 7.9 7.9 2 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL2323791 211976 None 0 Mouse Functional pEC50 = 6.0 6.0 4 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44441637 94102 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
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 94102 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
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 94185 None 0 Human Functional pEC50 = 6.0 6.0 -4 3
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 94185 None 0 Human Functional pEC50 = 6.0 6.0 -4 3
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 213684 None 0 Mouse Functional pEC50 = 5.0 5.0 1 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL2448525 212958 None 0 Mouse Functional pEC50 = 4.9 4.9 -177 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL102391 210914 None 0 Mouse Functional pEC50 = 4.9 4.9 2 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 199892 None 0 Mouse Functional pEC50 = 4.9 4.9 -2344 4
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 199892 None 0 Mouse Functional pEC50 = 4.9 4.9 -2344 4
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 140410 None 0 Human Functional pEC50 = 5.9 5.9 -45 4
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 140410 None 0 Human Functional pEC50 = 5.9 5.9 -45 4
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 173800 None 0 Mouse Functional pEC50 = 5.9 5.9 -50 3
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 173800 None 0 Mouse Functional pEC50 = 5.9 5.9 -50 3
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 155461 None 0 Human Functional pEC50 = 5.9 5.9 -9 3
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 155461 None 0 Human Functional pEC50 = 5.9 5.9 -9 3
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 156400 None 0 Mouse Functional pEC50 = 6.9 6.9 16 3
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 156400 None 0 Mouse Functional pEC50 = 6.9 6.9 16 3
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 156400 None 0 Mouse Functional pEC50 = 6.9 6.9 16 3
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 211969 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
168285801 191590 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
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 191590 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
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 185763 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
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 185763 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
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 31300 None 0 Human Functional pEC50 = 6.9 6.9 -295 3
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 31300 None 0 Human Functional pEC50 = 6.9 6.9 -295 3
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 199424 None 0 Mouse Functional pEC50 = 4.9 4.9 -7 3
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 199424 None 0 Mouse Functional pEC50 = 4.9 4.9 -7 3
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
155561743 175876 None 0 Mouse Functional pEC50 = 7.9 7.9 3 3
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 175876 None 0 Mouse Functional pEC50 = 7.9 7.9 3 3
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
155566298 175897 None 0 Mouse Functional pEC50 = 7.9 7.9 3 3
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 175897 None 0 Mouse Functional pEC50 = 7.9 7.9 3 3
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
164624151 185904 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 185904 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 186498 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 186498 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 158725 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 3
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 158725 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 3
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 174412 None 0 Mouse Functional pEC50 = 5.9 5.9 -18 2
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 174412 None 0 Mouse Functional pEC50 = 5.9 5.9 -18 2
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
CHEMBL2369131 212052 None 0 Mouse Functional pEC50 = 4.9 4.9 -3 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
137638778 156850 None 0 Human Functional pEC50 = 6.9 6.9 -81 3
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 156850 None 0 Human Functional pEC50 = 6.9 6.9 -81 3
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
145966490 164457 None 0 Human Functional pEC50 = 7.9 7.9 -3 4
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 164457 None 0 Human Functional pEC50 = 7.9 7.9 -3 4
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 164044 None 0 Human Functional pEC50 = 6.9 6.9 -23 4
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 164044 None 0 Human Functional pEC50 = 6.9 6.9 -23 4
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 186006 None 0 Mouse Functional pEC50 = 6.9 6.9 1 3
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 186006 None 0 Mouse Functional pEC50 = 6.9 6.9 1 3
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 173355 None 0 Mouse Functional pEC50 = 6.9 6.9 2 2
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 173355 None 0 Mouse Functional pEC50 = 6.9 6.9 2 2
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 215818 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
54584302 60832 None 0 Human Functional pEC50 = 5.9 5.9 -53 4
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 60832 None 0 Human Functional pEC50 = 5.9 5.9 -53 4
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 12285 None 0 Human Functional pEC50 = 5.9 5.9 -48 2
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 12285 None 0 Human Functional pEC50 = 5.9 5.9 -48 2
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
CHEMBL2028957 12285 None 0 Human Functional pEC50 = 5.9 5.9 -48 2
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 77191 None 0 Human Functional pEC50 = 5.9 5.9 -46 2
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
CHEMBL2028958 77191 None 0 Human Functional pEC50 = 5.9 5.9 -46 2
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 77191 None 0 Human Functional pEC50 = 5.9 5.9 -46 2
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 211943 None 0 Mouse Functional pEC50 = 5.9 5.9 -213 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL589515 218290 None 0 Mouse Functional pEC50 = 6.8 6.8 -2 3
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 None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmc.2009.12.010
46885368 7958 None 0 Human Functional pEC50 = 5.8 5.8 -13 3
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 7958 None 0 Human Functional pEC50 = 5.8 5.8 -13 3
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 205546 None 0 Mouse Functional pEC50 = 4.8 4.8 1 2
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 205546 None 0 Mouse Functional pEC50 = 4.8 4.8 1 2
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 122622 None 0 Human Functional pEC50 = 5.8 5.8 -8 4
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 122622 None 0 Human Functional pEC50 = 5.8 5.8 -8 4
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
16132144 211738 None 29 Mouse Functional pEC50 = 5.8 5.8 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
16133793 211738 None 29 Mouse Functional pEC50 = 5.8 5.8 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
44273719 211738 None 29 Mouse Functional pEC50 = 5.8 5.8 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 5.8 5.8 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
164610489 184661 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
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 184661 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
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 211912 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
46885863 8474 None 0 Human Functional pEC50 = 4.8 4.8 -41 2
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 8474 None 0 Human Functional pEC50 = 4.8 4.8 -41 2
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 214287 None 0 Human Functional pEC50 = 5.8 5.8 1 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184575 122493 None 0 Human Functional pEC50 = 5.8 5.8 -2 4
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 122493 None 0 Human Functional pEC50 = 5.8 5.8 -2 4
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 58821 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 3
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 58821 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 3
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 58821 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 3
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 58821 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 3
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 218308 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 3
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 None None None 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
162671821 183009 None 0 Mouse Functional pEC50 = 7.8 7.8 3 2
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 183009 None 0 Mouse Functional pEC50 = 7.8 7.8 3 2
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 157631 None 0 Mouse Functional pEC50 = 7.8 7.8 3 3
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 157631 None 0 Mouse Functional pEC50 = 7.8 7.8 3 3
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 214156 None 0 Mouse Functional pEC50 = 6.8 6.8 1 3
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
16725559 95042 None 0 Human Functional pEC50 = 5.8 5.8 -1230 4
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 95042 None 0 Human Functional pEC50 = 5.8 5.8 -1230 4
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 184867 None 0 Mouse Functional pEC50 = 5.8 5.8 6 2
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 184867 None 0 Mouse Functional pEC50 = 5.8 5.8 6 2
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 157179 None 0 Mouse Functional pEC50 = 4.8 4.8 -36 2
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 157179 None 0 Mouse Functional pEC50 = 4.8 4.8 -36 2
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
171378343 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
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 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
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 203511 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
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 203511 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
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 199830 None 0 Mouse Functional pEC50 = 4.8 4.8 -9 3
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 199830 None 0 Mouse Functional pEC50 = 4.8 4.8 -9 3
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 95652 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 95652 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 216096 None 2 Mouse Functional pEC50 = 5.8 5.8 1 4
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None 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 214286 None 0 Human Functional pEC50 = 5.8 5.8 -17 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600832 214273 None 0 Human Functional pEC50 = 6.8 6.8 -3 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371965 212621 None 0 Human Functional pEC50 = 7.8 7.8 331 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
132180597 156262 None 0 Mouse Functional pEC50 = 7.8 7.8 -23 3
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 156262 None 0 Mouse Functional pEC50 = 7.8 7.8 -23 3
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
16132144 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16133793 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
44273719 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16132144 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16133793 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
44273719 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16132144 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
16133793 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44273719 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.8 7.8 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL451423 216431 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
145964017 164136 None 0 Human Functional pEC50 = 6.8 6.8 -10 4
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 164136 None 0 Human Functional pEC50 = 6.8 6.8 -10 4
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
1324 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
16154396 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
16197727 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
16197727.0 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
44285019 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
57514683 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
91898441 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
DB04931 302 None 19 Mouse Functional pEC50 = 6.8 6.8 -5 8
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 None None None None 10.1016/s0960-894x(03)00318-4
10146211 64350 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
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 64350 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
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
44347221 16642 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 16642 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 175471 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
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 175471 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
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 184603 None 0 Mouse Functional pEC50 = 5.8 5.8 3 2
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 184603 None 0 Mouse Functional pEC50 = 5.8 5.8 3 2
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 97954 None 0 Mouse Functional pEC50 = 4.8 4.8 -9 2
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 97954 None 0 Mouse Functional pEC50 = 4.8 4.8 -9 2
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 154177 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 154177 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 199812 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
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 199812 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
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 7862 None 0 Human Functional pEC50 = 4.8 4.8 -389 3
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 7862 None 0 Human Functional pEC50 = 4.8 4.8 -389 3
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 164442 None 0 Human Functional pEC50 = 7.8 7.8 -3 4
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 164442 None 0 Human Functional pEC50 = 7.8 7.8 -3 4
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 159804 None 0 Mouse Functional pEC50 = 7.8 7.8 1 3
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 159804 None 0 Mouse Functional pEC50 = 7.8 7.8 1 3
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 182336 None 0 Mouse Functional pEC50 = 7.8 7.8 -16 2
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 182336 None 0 Mouse Functional pEC50 = 7.8 7.8 -16 2
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
155558348 175140 None 0 Mouse Functional pEC50 = 7.8 7.8 5 3
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 175140 None 0 Mouse Functional pEC50 = 7.8 7.8 5 3
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
132180653 175163 None 0 Mouse Functional pEC50 = 7.8 7.8 -17 2
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 175163 None 0 Mouse Functional pEC50 = 7.8 7.8 -17 2
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
CHEMBL420167 215702 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 None None None NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL427205 215813 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
164624627 185985 None 0 Mouse Functional pEC50 = 6.8 6.8 2 3
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 185985 None 0 Mouse Functional pEC50 = 6.8 6.8 2 3
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 146012 None 0 Human Functional pEC50 = 6.8 6.8 -5 4
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 146012 None 0 Human Functional pEC50 = 6.8 6.8 -5 4
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 8278 None 0 Human Functional pEC50 = 5.8 5.8 -295 3
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 8278 None 0 Human Functional pEC50 = 5.8 5.8 -295 3
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 186619 None 0 Mouse Functional pEC50 = 5.8 5.8 1 3
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 186619 None 0 Mouse Functional pEC50 = 5.8 5.8 1 3
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 213864 None 0 Human Functional pEC50 = 5.8 5.8 -8 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
71449119 78999 None 0 Human Functional pEC50 = 5.8 5.8 -117 2
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 78999 None 0 Human Functional pEC50 = 5.8 5.8 -117 2
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 172893 None 0 Mouse Functional pEC50 = 5.8 5.8 1 2
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 172893 None 0 Mouse Functional pEC50 = 5.8 5.8 1 2
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 157600 None 0 Mouse Functional pEC50 = 4.8 4.8 -10 2
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 157600 None 0 Mouse Functional pEC50 = 4.8 4.8 -10 2
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 199817 None 0 Mouse Functional pEC50 = 4.7 4.7 -10 2
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 199817 None 0 Mouse Functional pEC50 = 4.7 4.7 -10 2
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 211945 None 0 Mouse Functional pEC50 = 4.7 4.7 -2 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL431242 216085 None 0 Mouse Functional pEC50 = 4.7 4.7 1 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 199310 None 0 Mouse Functional pEC50 = 4.7 4.7 -5 3
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 199310 None 0 Mouse Functional pEC50 = 4.7 4.7 -5 3
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 184671 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 184671 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 213228 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
71449047 78511 None 0 Human Functional pEC50 = 6.7 6.7 -40 3
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 78511 None 0 Human Functional pEC50 = 6.7 6.7 -40 3
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 11804 None 0 Human Functional pEC50 = 5.7 5.7 -72 2
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 11804 None 0 Human Functional pEC50 = 5.7 5.7 -72 2
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
CHEMBL2028961 11804 None 0 Human Functional pEC50 = 5.7 5.7 -72 2
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
6918813 131439 None 2 Human Functional pEC50 = 5.7 5.7 -398 4
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 131439 None 2 Human Functional pEC50 = 5.7 5.7 -398 4
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 199829 None 0 Mouse Functional pEC50 = 4.7 4.7 -6 3
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 199829 None 0 Mouse Functional pEC50 = 4.7 4.7 -6 3
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 7962 None 25 Human Functional pEC50 = 5.7 5.7 -165 4
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 7962 None 25 Human Functional pEC50 = 5.7 5.7 -165 4
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
CHEMBL1204059 7962 None 25 Human Functional pEC50 = 5.7 5.7 -165 4
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 94058 None 0 Human Functional pEC50 = 5.7 5.7 -43 2
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 94058 None 0 Human Functional pEC50 = 5.7 5.7 -43 2
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 67453 None 0 Human Functional pEC50 = 5.7 5.7 -43 3
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 67453 None 0 Human Functional pEC50 = 5.7 5.7 -43 3
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 211942 None 0 Mouse Functional pEC50 = 4.7 4.7 -3 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
145971389 164728 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
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 164728 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
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 98017 None 0 Mouse Functional pEC50 = 8.7 8.7 1 4
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 98017 None 0 Mouse Functional pEC50 = 8.7 8.7 1 4
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
16132144 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
16133793 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
44273719 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -1 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
CHEMBL444219 216391 None 0 Mouse Functional pEC50 = 8.7 8.7 -4 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
127046235 139725 None 0 Mouse Functional pEC50 = 8.7 8.7 2 4
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 139725 None 0 Mouse Functional pEC50 = 8.7 8.7 2 4
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 159120 None 0 Mouse Functional pEC50 = 8.7 8.7 5 3
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 159120 None 0 Mouse Functional pEC50 = 8.7 8.7 5 3
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
155543031 173284 None 0 Mouse Functional pEC50 = 8.7 8.7 -3 3
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 173284 None 0 Mouse Functional pEC50 = 8.7 8.7 -3 3
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 215086 None 0 Mouse Functional pEC50 = 8.7 8.7 2 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL1688107 211293 None 0 Mouse Functional pEC50 = 8.6 8.6 -8 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
1325 3600 None 12 Mouse Functional pEC50 = 8.6 8.6 -3 4
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 None None None None 10.1021/acs.jmedchem.5b00184
6440621 3600 None 12 Mouse Functional pEC50 = 8.6 8.6 -3 4
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 None None None None 10.1021/acs.jmedchem.5b00184
9898183 3600 None 12 Mouse Functional pEC50 = 8.6 8.6 -3 4
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 None None None None 10.1021/acs.jmedchem.5b00184
CHEMBL3422426 3600 None 12 Mouse Functional pEC50 = 8.6 8.6 -3 4
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 None None None None 10.1021/acs.jmedchem.5b00184
CHEMBL3287327 213769 None 0 Mouse Functional pEC50 = 8.6 8.6 1 4
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
44400428 125744 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 3
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 125744 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 3
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 168958 None 0 Human Functional pEC50 = 8.6 8.6 4 4
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 168958 None 0 Human Functional pEC50 = 8.6 8.6 4 4
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 216637 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1324 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
16154396 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
16197727 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
16197727.0 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
44285019 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
57514683 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
91898441 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
DB04931 302 None 19 Mouse Functional pEC50 = 8.6 8.6 -5 8
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 None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL370254 214626 None 2 Mouse Functional pEC50 = 8.6 8.6 6 3
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm0490843
11263053 68042 None 0 Mouse Functional pEC50 = 8.6 8.6 -3 3
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 68042 None 0 Mouse Functional pEC50 = 8.6 8.6 -3 3
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 216421 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
11423083 96892 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 3
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 96892 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 3
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
145948876 167581 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
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 167581 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
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 156782 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 3
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 156782 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 3
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 211625 None 0 Human Functional pEC50 = 6.7 6.7 -4 4
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
137651071 157559 None 0 Mouse Functional pEC50 = 6.7 6.7 -25 3
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 157559 None 0 Mouse Functional pEC50 = 6.7 6.7 -25 3
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 216270 None 0 Human Functional pEC50 = 6.7 6.7 -26 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL433645 216104 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 None None None NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL409636 215233 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
CHEMBL375947 214692 None 0 Human Functional pEC50 = 5.7 5.7 -1 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155512534 169795 None 0 Mouse Functional pEC50 = 5.7 5.7 -22 3
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 169795 None 0 Mouse Functional pEC50 = 5.7 5.7 -22 3
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 213685 None 0 Mouse Functional pEC50 = 5.7 5.7 1 3
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 None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44391940 12254 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 12254 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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
CHEMBL2145456 12254 None 0 Human Functional pEC50 = 5.7 5.7 -21 2
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 8472 None 0 Human Functional pEC50 = 4.7 4.7 -27 2
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 8472 None 0 Human Functional pEC50 = 4.7 4.7 -27 2
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
CHEMBL1204065 8472 None 0 Human Functional pEC50 = 4.7 4.7 -27 2
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 102869 None 0 Mouse Functional pEC50 = 4.7 4.7 -1 2
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 102869 None 0 Mouse Functional pEC50 = 4.7 4.7 -1 2
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 29083 None 0 Mouse Functional pEC50 = 4.7 4.7 -2 2
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 29083 None 0 Mouse Functional pEC50 = 4.7 4.7 -2 2
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 184730 None 0 Mouse Functional pEC50 = 5.7 5.7 11 2
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 184730 None 0 Mouse Functional pEC50 = 5.7 5.7 11 2
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 211978 None 0 Mouse Functional pEC50 = 6.7 6.7 -27 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44335147 4594 None 0 Mouse Functional pEC50 = 5.7 5.7 4 3
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 4594 None 0 Mouse Functional pEC50 = 5.7 5.7 4 3
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 218113 None 0 Human Functional pEC50 = 7.7 7.7 3 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
54587278 60838 None 0 Human Functional pEC50 = 6.7 6.7 -138 4
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 60838 None 0 Human Functional pEC50 = 6.7 6.7 -138 4
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 156894 None 0 Mouse Functional pEC50 = 6.7 6.7 -3 3
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 156894 None 0 Mouse Functional pEC50 = 6.7 6.7 -3 3
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 63487 None 0 Human Functional pEC50 = 6.7 6.7 -204 2
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 63487 None 0 Human Functional pEC50 = 6.7 6.7 -204 2
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 168543 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 168543 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 212427 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL607104 218318 None 0 Mouse Functional pEC50 = 4.7 4.7 2 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 185673 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 185673 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 216466 None 0 Mouse Functional pEC50 = 7.7 7.7 4 2
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 None None None CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 6.7 6.7 -8 6
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 None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44347331 16334 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 16334 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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
44441641 94354 None 0 Human Functional pEC50 = 6.7 6.7 -134 3
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 94354 None 0 Human Functional pEC50 = 6.7 6.7 -134 3
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 213929 None 0 Mouse Functional pEC50 = 5.7 5.7 -13 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
44310258 159512 None 0 Mouse Functional pEC50 = 5.7 5.7 2 3
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 159512 None 0 Mouse Functional pEC50 = 5.7 5.7 2 3
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 159512 None 0 Mouse Functional pEC50 = 5.7 5.7 2 3
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 216605 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
45487413 199707 None 0 Mouse Functional pEC50 = 5.6 5.6 -1 3
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 199707 None 0 Mouse Functional pEC50 = 5.6 5.6 -1 3
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 154394 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 154394 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 184491 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
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 184491 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
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 64243 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 64243 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 200105 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
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 200105 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
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 203513 None 0 Mouse Functional pEC50 = 5.6 5.6 -2 2
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 203513 None 0 Mouse Functional pEC50 = 5.6 5.6 -2 2
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 199815 None 0 Mouse Functional pEC50 = 4.6 4.6 -7 3
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 199815 None 0 Mouse Functional pEC50 = 4.6 4.6 -7 3
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 122502 None 0 Human Functional pEC50 = 6.6 6.6 -1 4
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 122502 None 0 Human Functional pEC50 = 6.6 6.6 -1 4
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
155565321 175680 None 0 Mouse Functional pEC50 = 6.6 6.6 -7 3
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 175680 None 0 Mouse Functional pEC50 = 6.6 6.6 -7 3
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 16334 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 16334 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 218036 None 0 Human Functional pEC50 = 5.6 5.6 -6 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44401585 13768 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 13768 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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
CHEMBL554368 13768 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 79005 None 0 Human Functional pEC50 = 5.6 5.6 -57 4
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 79005 None 0 Human Functional pEC50 = 5.6 5.6 -57 4
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
155548791 173834 None 0 Mouse Functional pEC50 = 5.6 5.6 -30 3
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 173834 None 0 Mouse Functional pEC50 = 5.6 5.6 -30 3
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
162670795 182932 None 0 Mouse Functional pEC50 = 7.6 7.6 -14 2
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 182932 None 0 Mouse Functional pEC50 = 7.6 7.6 -14 2
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
1323 2688 None 38 Human Functional pEC50 = 7.6 7.6 -181 7
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
92432 2688 None 38 Human Functional pEC50 = 7.6 7.6 -181 7
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.6 7.6 -181 7
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
137649368 157498 None 0 Mouse Functional pEC50 = 6.6 6.6 -35 3
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 157498 None 0 Mouse Functional pEC50 = 6.6 6.6 -35 3
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 154928 None 0 Human Functional pEC50 = 6.6 6.6 -66 3
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 154928 None 0 Human Functional pEC50 = 6.6 6.6 -66 3
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 211957 None 0 Human Functional pEC50 = 6.6 6.6 -20 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL455070 216468 None 0 Human Functional pEC50 = 5.6 5.6 -25 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44457067 97795 None 0 Mouse Functional pEC50 = 7.6 7.6 -5 4
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 97795 None 0 Mouse Functional pEC50 = 7.6 7.6 -5 4
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 180750 None 0 Mouse Functional pEC50 = 7.6 7.6 -29 2
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 180750 None 0 Mouse Functional pEC50 = 7.6 7.6 -29 2
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 156322 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
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 156322 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
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 4594 None 0 Mouse Functional pEC50 = 6.6 6.6 4 3
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 4594 None 0 Mouse Functional pEC50 = 6.6 6.6 4 3
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
CHEMBL3350396 213938 None 0 Human Functional pEC50 = 6.6 6.6 -371 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL376614 214712 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL2323790 211975 None 0 Mouse Functional pEC50 = 6.6 6.6 -8 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137653916 158672 None 0 Mouse Functional pEC50 = 6.6 6.6 -3 3
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 158672 None 0 Mouse Functional pEC50 = 6.6 6.6 -3 3
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 176152 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
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 176152 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
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 213057 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44392015 12782 None 0 Human Functional pEC50 = 5.6 5.6 -41 2
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 12782 None 0 Human Functional pEC50 = 5.6 5.6 -41 2
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
CHEMBL3216179 12782 None 0 Human Functional pEC50 = 5.6 5.6 -41 2
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
1338 3807 None 36 Human Functional pEC50 = 5.6 5.6 -660 8
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 3807 None 36 Human Functional pEC50 = 5.6 5.6 -660 8
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 3807 None 36 Human Functional pEC50 = 5.6 5.6 -660 8
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 173551 None 0 Mouse Functional pEC50 = 4.6 4.6 -1 2
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 173551 None 0 Mouse Functional pEC50 = 4.6 4.6 -1 2
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 115264 None 2 Human Functional pEC50 = 6.6 6.6 -128 2
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(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1 10.1021/jm025539h
CHEMBL334457 115264 None 2 Human Functional pEC50 = 6.6 6.6 -128 2
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(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1 10.1021/jm025539h
45487411 199501 None 0 Mouse Functional pEC50 = 5.6 5.6 -10 3
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 199501 None 0 Mouse Functional pEC50 = 5.6 5.6 -10 3
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 213142 None 0 Human Functional pEC50 = 7.6 7.6 -776 6
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL2370963 212425 None 0 Human Functional pEC50 = 7.6 7.6 85 2
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44408190 96976 None 0 Human Functional pEC50 = 6.6 6.6 -46 4
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 96976 None 0 Human Functional pEC50 = 6.6 6.6 -46 4
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 15036 None 0 Human Functional pEC50 = 5.6 5.6 -42 4
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 15036 None 0 Human Functional pEC50 = 5.6 5.6 -42 4
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 216082 None 0 Mouse Functional pEC50 = 5.6 5.6 2 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 121321 None 0 Mouse Functional pEC50 = 4.6 4.6 -2 2
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 121321 None 0 Mouse Functional pEC50 = 4.6 4.6 -2 2
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 175053 None 0 Mouse Functional pEC50 = 4.6 4.6 -15 2
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 175053 None 0 Mouse Functional pEC50 = 4.6 4.6 -15 2
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 205544 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 205544 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 211971 None 0 Mouse Functional pEC50 = 7.5 7.5 -2 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
16132144 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
16133793 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
44273719 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
137646614 157630 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 2
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 157630 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 2
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 195974 None 0 Human Functional pEC50 = 6.5 6.5 -2187 4
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 195974 None 0 Human Functional pEC50 = 6.5 6.5 -2187 4
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 203512 None 0 Mouse Functional pEC50 = 5.5 5.5 -4 3
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 203512 None 0 Mouse Functional pEC50 = 5.5 5.5 -4 3
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 154781 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
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 154781 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
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 156000 None 0 Human Functional pEC50 = 6.5 6.5 -72 3
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 156000 None 0 Human Functional pEC50 = 6.5 6.5 -72 3
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 213067 None 0 Mouse Functional pEC50 = 8.5 8.5 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
90643805 111808 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 4
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 111808 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 4
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 173435 None 0 Mouse Functional pEC50 = 8.5 8.5 1 2
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 173435 None 0 Mouse Functional pEC50 = 8.5 8.5 1 2
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 173981 None 0 Mouse Functional pEC50 = 8.5 8.5 -7 3
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 173981 None 0 Mouse Functional pEC50 = 8.5 8.5 -7 3
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 174018 None 0 Mouse Functional pEC50 = 8.5 8.5 5 3
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 174018 None 0 Mouse Functional pEC50 = 8.5 8.5 5 3
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 69415 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 3
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 69415 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 3
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 213067 None 0 Mouse Functional pEC50 = 8.5 8.5 2 7
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
127047475 139836 None 0 Mouse Functional pEC50 = 8.5 8.5 1 4
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 139836 None 0 Mouse Functional pEC50 = 8.5 8.5 1 4
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 139836 None 0 Mouse Functional pEC50 = 8.5 8.5 1 4
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 216286 None 0 Human Functional pEC50 = 8.5 8.5 1 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL3358533 214026 None 0 Mouse Functional pEC50 = 8.5 8.5 -7 3
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 None None None C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.5 8.5 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm070461w
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm070461w
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm801300c
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/jm801300c
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -181 7
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 None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL393075 214922 None 0 Human Functional pEC50 = 8.5 8.5 -20 4
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 None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
11239907 133195 None 0 Mouse Functional pEC50 = 8.5 8.5 -5 3
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 133195 None 0 Mouse Functional pEC50 = 8.5 8.5 -5 3
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
155564058 175438 None 0 Mouse Functional pEC50 = 8.5 8.5 -16 3
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 175438 None 0 Mouse Functional pEC50 = 8.5 8.5 -16 3
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 213067 None 0 Mouse Functional pEC50 = 8.5 8.5 2 7
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
162673830 183265 None 0 Mouse Functional pEC50 = 8.5 8.5 -15 2
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 183265 None 0 Mouse Functional pEC50 = 8.5 8.5 -15 2
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 212426 None 0 Human Functional pEC50 = 8.4 8.4 -10 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL4299619 216056 None 0 Mouse Functional pEC50 = 8.4 8.4 2 3
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 None None None CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL2370964 212426 None 0 Human Functional pEC50 = 8.4 8.4 -10 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL264190 213067 None 0 Human Functional pEC50 = 8.4 8.4 -3 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL264190 213067 None 0 Human Functional pEC50 = 8.4 8.4 -3 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.2c01794
127047913 140011 None 0 Mouse Functional pEC50 = 8.4 8.4 4 4
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 140011 None 0 Mouse Functional pEC50 = 8.4 8.4 4 4
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 213067 None 0 Mouse Functional pEC50 = 8.4 8.4 2 7
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
164612516 185499 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
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 185499 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
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 218077 None 0 Mouse Functional pEC50 = 7.5 7.5 -3 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
155556047 174601 None 0 Mouse Functional pEC50 = 7.5 7.5 1 3
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 174601 None 0 Mouse Functional pEC50 = 7.5 7.5 1 3
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 211619 None 0 Human Functional pEC50 = 6.5 6.5 1 3
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
155531140 171721 None 0 Mouse Functional pEC50 = 6.5 6.5 1 3
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 171721 None 0 Mouse Functional pEC50 = 6.5 6.5 1 3
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 12799 None 0 Human Functional pEC50 = 6.5 6.5 -51 2
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 12799 None 0 Human Functional pEC50 = 6.5 6.5 -51 2
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
CHEMBL535152 12799 None 0 Human Functional pEC50 = 6.5 6.5 -51 2
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 114487 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 114487 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 199893 None 0 Mouse Functional pEC50 = 4.5 4.5 -25 3
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 199893 None 0 Mouse Functional pEC50 = 4.5 4.5 -25 3
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 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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
44305790 102895 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 102895 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 199269 None 0 Mouse Functional pEC50 = 5.5 5.5 -3 3
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 199269 None 0 Mouse Functional pEC50 = 5.5 5.5 -3 3
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 212629 None 0 Human Functional pEC50 = 7.5 7.5 57 2
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
162661724 181641 None 0 Mouse Functional pEC50 = 7.5 7.5 2 2
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 181641 None 0 Mouse Functional pEC50 = 7.5 7.5 2 2
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
162664463 182296 None 0 Mouse Functional pEC50 = 7.5 7.5 5 2
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 182296 None 0 Mouse Functional pEC50 = 7.5 7.5 5 2
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
46232223 201620 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 201620 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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
CHEMBL302703 213373 None 0 Mouse Functional pEC50 = 6.5 6.5 9 4
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
46232228 203480 None 0 Mouse Functional pEC50 = 6.5 6.5 3 3
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 203480 None 0 Mouse Functional pEC50 = 6.5 6.5 3 3
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 97457 None 0 Mouse Functional pEC50 = 5.5 5.5 2 3
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 97457 None 0 Mouse Functional pEC50 = 5.5 5.5 2 3
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 210924 None 0 Mouse Functional pEC50 = 4.5 4.5 1 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 205795 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 205795 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
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 94107 None 0 Human Functional pEC50 = 7.5 7.5 -83 4
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 94107 None 0 Human Functional pEC50 = 7.5 7.5 -83 4
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
1323 2688 None 38 Human Functional pEC50 = 7.5 7.5 -181 7
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 None None None None 10.1021/acs.jmedchem.7b00353
92432 2688 None 38 Human Functional pEC50 = 7.5 7.5 -181 7
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 None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.5 7.5 -181 7
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 None None None None 10.1021/acs.jmedchem.7b00353
137645483 157710 None 0 Mouse Functional pEC50 = 6.5 6.5 1 3
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 157710 None 0 Mouse Functional pEC50 = 6.5 6.5 1 3
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 13996 None 0 Human Functional pEC50 = 5.5 5.5 -66 3
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 13996 None 0 Human Functional pEC50 = 5.5 5.5 -66 3
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
CHEMBL3216393 13996 None 0 Human Functional pEC50 = 5.5 5.5 -66 3
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 58820 None 0 Mouse Functional pEC50 = 6.5 6.5 -2 3
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 58820 None 0 Mouse Functional pEC50 = 6.5 6.5 -2 3
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 210918 None 0 Mouse Functional pEC50 = 7.5 7.5 -2 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44408286 140755 None 0 Human Functional pEC50 = 6.5 6.5 -117 4
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 140755 None 0 Human Functional pEC50 = 6.5 6.5 -117 4
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 159665 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 3
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 159665 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 3
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 216562 None 0 Mouse Functional pEC50 = 6.5 6.5 -3 3
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 None None None 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 185660 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 185660 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
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 12788 None 0 Human Functional pEC50 = 6.5 6.5 -97 2
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 12788 None 0 Human Functional pEC50 = 6.5 6.5 -97 2
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
CHEMBL534928 12788 None 0 Human Functional pEC50 = 6.5 6.5 -97 2
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 11750 None 0 Human Functional pEC50 = 6.5 6.5 -20 2
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 11750 None 0 Human Functional pEC50 = 6.5 6.5 -20 2
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
CHEMBL2145455 11750 None 0 Human Functional pEC50 = 6.5 6.5 -20 2
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
45487417 199500 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 3
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 199500 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 3
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
CHEMBL602650 218307 None 0 Mouse Functional pEC50 = 5.5 5.5 2 3
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 None None None 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
16157270 215013 None 15 Mouse Functional pEC50 = 7.5 7.5 -22 6
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/acs.jmedchem.5b01894
CHEMBL405282 215013 None 15 Mouse Functional pEC50 = 7.5 7.5 -22 6
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/acs.jmedchem.5b01894
16132144 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
16133793 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
44273719 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.5 7.5 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL2323799 211984 None 0 Mouse Functional pEC50 = 6.5 6.5 -22 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
46232225 203539 None 0 Mouse Functional pEC50 = 6.5 6.5 4 3
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 203539 None 0 Mouse Functional pEC50 = 6.5 6.5 4 3
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 8030 None 0 Human Functional pEC50 = 5.5 5.5 -56 4
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 8030 None 0 Human Functional pEC50 = 5.5 5.5 -56 4
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 216366 None 2 Mouse Functional pEC50 = 7.4 7.4 162 2
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 None None None 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
162665266 182287 None 0 Mouse Functional pEC50 = 7.4 7.4 4 2
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 182287 None 0 Mouse Functional pEC50 = 7.4 7.4 4 2
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 214893 None 0 Human Functional pEC50 = 6.4 6.4 1 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
16132144 211738 None 29 Human Functional pEC50 = 6.4 6.4 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
16133793 211738 None 29 Human Functional pEC50 = 6.4 6.4 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
44273719 211738 None 29 Human Functional pEC50 = 6.4 6.4 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
CHEMBL214332 211738 None 29 Human Functional pEC50 = 6.4 6.4 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
CHEMBL138771 211213 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None 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 13994 None 0 Human Functional pEC50 = 6.4 6.4 -61 2
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 13994 None 0 Human Functional pEC50 = 6.4 6.4 -61 2
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
CHEMBL558787 13994 None 0 Human Functional pEC50 = 6.4 6.4 -61 2
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 140431 None 0 Human Functional pEC50 = 5.4 5.4 -141 4
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 140431 None 0 Human Functional pEC50 = 5.4 5.4 -141 4
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 8073 None 0 Human Functional pEC50 = 5.4 5.4 -204 4
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 8073 None 0 Human Functional pEC50 = 5.4 5.4 -204 4
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
CHEMBL1204061 8073 None 0 Human Functional pEC50 = 5.4 5.4 -204 4
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 210921 None 0 Mouse Functional pEC50 = 4.4 4.4 -1 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 8121 None 0 Human Functional pEC50 = 5.4 5.4 -52 4
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 8121 None 0 Human Functional pEC50 = 5.4 5.4 -52 4
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 166591 None 0 Human Functional pEC50 = 7.4 7.4 1 4
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 166591 None 0 Human Functional pEC50 = 7.4 7.4 1 4
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 195257 None 0 Human Functional pEC50 = 6.4 6.4 -831 4
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 195257 None 0 Human Functional pEC50 = 6.4 6.4 -831 4
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 95026 None 0 Human Functional pEC50 = 6.4 6.4 -245 4
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 95026 None 0 Human Functional pEC50 = 6.4 6.4 -245 4
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 156329 None 0 Human Functional pEC50 = 6.4 6.4 -40 3
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 156329 None 0 Human Functional pEC50 = 6.4 6.4 -40 3
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 186596 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
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 186596 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
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 154890 None 0 Human Functional pEC50 = 6.4 6.4 -43 2
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 154890 None 0 Human Functional pEC50 = 6.4 6.4 -43 2
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 157368 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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 157368 None 0 Human Functional pEC50 = 6.4 6.4 1 3
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
162662213 181602 None 0 Mouse Functional pEC50 = 7.4 7.4 3 2
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 181602 None 0 Mouse Functional pEC50 = 7.4 7.4 3 2
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 97665 None 0 Mouse Functional pEC50 = 6.4 6.4 -3 4
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 97665 None 0 Mouse Functional pEC50 = 6.4 6.4 -3 4
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
51350799 58818 None 0 Mouse Functional pEC50 = 6.4 6.4 3 3
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 58818 None 0 Mouse Functional pEC50 = 6.4 6.4 3 3
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 58818 None 0 Mouse Functional pEC50 = 6.4 6.4 3 3
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 58818 None 0 Mouse Functional pEC50 = 6.4 6.4 3 3
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
1334 1501 None 4 Human Functional pEC50 = 6.4 6.4 -17 4
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 None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Functional pEC50 = 6.4 6.4 -17 4
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 None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.4 6.4 -17 4
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 None None None None 10.1021/jm049579s
44310243 169290 None 0 Mouse Functional pEC50 = 5.4 5.4 2 3
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 169290 None 0 Mouse Functional pEC50 = 5.4 5.4 2 3
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 169290 None 0 Mouse Functional pEC50 = 5.4 5.4 2 3
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
46232221 201625 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 3
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 201625 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 3
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
44305805 100936 None 0 Mouse Functional pEC50 = 4.4 4.4 1 2
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 100936 None 0 Mouse Functional pEC50 = 4.4 4.4 1 2
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 213067 None 0 Mouse Functional pEC50 = 8.4 8.4 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
127047853 140080 None 0 Mouse Functional pEC50 = 8.4 8.4 4 4
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 140080 None 0 Mouse Functional pEC50 = 8.4 8.4 4 4
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 213067 None 0 Mouse Functional pEC50 = 8.4 8.4 2 7
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
155539948 172989 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 3
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 172989 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 3
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 212430 None 0 Human Functional pEC50 = 8.4 8.4 -1 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370968 212430 None 0 Human Functional pEC50 = 8.4 8.4 -1 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.4 8.4 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.0c02041
CHEMBL385465 214811 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 None None None CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL405791 215040 None 0 Mouse Functional pEC50 = 8.4 8.4 1 4
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ncc[nH]2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
11491374 67641 None 0 Mouse Functional pEC50 = 8.4 8.4 -4 3
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 67641 None 0 Mouse Functional pEC50 = 8.4 8.4 -4 3
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 176070 None 0 Mouse Functional pEC50 = 8.3 8.3 17 3
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 176070 None 0 Mouse Functional pEC50 = 8.3 8.3 17 3
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 166252 None 0 Mouse Functional pEC50 = 8.3 8.3 -1 3
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 166252 None 0 Mouse Functional pEC50 = 8.3 8.3 -1 3
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 214728 None 0 Mouse Functional pEC50 = 8.3 8.3 8 4
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 None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
137644449 158384 None 0 Mouse Functional pEC50 = 7.4 7.4 3 3
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 158384 None 0 Mouse Functional pEC50 = 7.4 7.4 3 3
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 173181 None 0 Mouse Functional pEC50 = 7.4 7.4 -199 3
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 173181 None 0 Mouse Functional pEC50 = 7.4 7.4 -199 3
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 173960 None 0 Mouse Functional pEC50 = 7.4 7.4 10 3
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 173960 None 0 Mouse Functional pEC50 = 7.4 7.4 10 3
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 75412 None 0 Human Functional pEC50 = 6.4 6.4 -162 4
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 75412 None 0 Human Functional pEC50 = 6.4 6.4 -162 4
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 75446 None 0 Human Functional pEC50 = 6.4 6.4 -47 4
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 75446 None 0 Human Functional pEC50 = 6.4 6.4 -47 4
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 213758 None 0 Mouse Functional pEC50 = 6.4 6.4 -6 4
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 None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL317228 213659 None 0 Mouse Functional pEC50 = 5.4 5.4 3 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)c1ccccc1 10.1021/jm010524p
155558598 174864 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 2
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 174864 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 2
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 211667 None 0 Human Functional pEC50 = 6.4 6.4 -23 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
137640715 157095 None 0 Mouse Functional pEC50 = 5.4 5.4 -56 2
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 157095 None 0 Mouse Functional pEC50 = 5.4 5.4 -56 2
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 118864 None 0 Human Functional pEC50 = 5.4 5.4 -91 4
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 118864 None 0 Human Functional pEC50 = 5.4 5.4 -91 4
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 210920 None 0 Mouse Functional pEC50 = 4.4 4.4 -1 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 211974 None 0 Mouse Functional pEC50 = 6.4 6.4 -213 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2370553 212329 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
155566074 175838 None 0 Mouse Functional pEC50 = 5.4 5.4 -13 2
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 175838 None 0 Mouse Functional pEC50 = 5.4 5.4 -13 2
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 210933 None 0 Mouse Functional pEC50 = 5.4 5.4 -2 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm010524p
145989222 167376 None 0 Human Functional pEC50 = 6.4 6.4 -25 4
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 167376 None 0 Human Functional pEC50 = 6.4 6.4 -25 4
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 97625 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 97625 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 188843 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
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 188843 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
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 186714 None 0 Mouse Functional pEC50 = 6.4 6.4 18 3
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 186714 None 0 Mouse Functional pEC50 = 6.4 6.4 18 3
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
137657607 159730 None 0 Mouse Functional pEC50 = 5.4 5.4 -81 2
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 159730 None 0 Mouse Functional pEC50 = 5.4 5.4 -81 2
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 122494 None 0 Human Functional pEC50 = 6.4 6.4 -32 4
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 122494 None 0 Human Functional pEC50 = 6.4 6.4 -32 4
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 12291 None 0 Human Functional pEC50 = 7.4 7.4 1 2
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 12291 None 0 Human Functional pEC50 = 7.4 7.4 1 2
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
CHEMBL2028956 12291 None 0 Human Functional pEC50 = 7.4 7.4 1 2
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 12965 None 0 Human Functional pEC50 = 6.4 6.4 -181 3
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 12965 None 0 Human Functional pEC50 = 6.4 6.4 -181 3
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
CHEMBL538567 12965 None 0 Human Functional pEC50 = 6.4 6.4 -181 3
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 215264 None 0 Human Functional pEC50 = 6.4 6.4 -50 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44448631 95123 None 0 Human Functional pEC50 = 6.3 6.3 -91 4
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 95123 None 0 Human Functional pEC50 = 6.3 6.3 -91 4
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
102096778 58823 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 58823 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 58823 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 58823 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 58823 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 211979 None 0 Mouse Functional pEC50 = 7.3 7.3 -5 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137638218 156920 None 0 Mouse Functional pEC50 = 7.3 7.3 2 3
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 156920 None 0 Mouse Functional pEC50 = 7.3 7.3 2 3
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 212683 None 0 Mouse Functional pEC50 = 7.3 7.3 1 3
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC(C)(C)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
44408189 168982 None 0 Human Functional pEC50 = 6.3 6.3 -32 4
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 168982 None 0 Human Functional pEC50 = 6.3 6.3 -32 4
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 214277 None 0 Human Functional pEC50 = 6.3 6.3 -1 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2323798 211983 None 0 Mouse Functional pEC50 = 6.3 6.3 -15 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCN)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2304248 211944 None 0 Mouse Functional pEC50 = 5.3 5.3 -2 3
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 None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
164614821 185374 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 185374 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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
45487285 199449 None 0 Mouse Functional pEC50 = 5.3 5.3 -7 2
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 199449 None 0 Mouse Functional pEC50 = 5.3 5.3 -7 2
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 192351 None 0 Human Functional pEC50 = 7.3 7.3 -7 4
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 192351 None 0 Human Functional pEC50 = 7.3 7.3 -7 4
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 158689 None 0 Mouse Functional pEC50 = 7.3 7.3 3 3
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 158689 None 0 Mouse Functional pEC50 = 7.3 7.3 3 3
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 140756 None 0 Human Functional pEC50 = 6.3 6.3 -30 4
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 140756 None 0 Human Functional pEC50 = 6.3 6.3 -30 4
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 185699 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 185699 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 94065 None 0 Human Functional pEC50 = 6.3 6.3 -6 2
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 94065 None 0 Human Functional pEC50 = 6.3 6.3 -6 2
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 201626 None 0 Mouse Functional pEC50 = 6.3 6.3 2 3
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 201626 None 0 Mouse Functional pEC50 = 6.3 6.3 2 3
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 213864 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
49862375 15045 None 0 Human Functional pEC50 = 6.3 6.3 -16 4
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 15045 None 0 Human Functional pEC50 = 6.3 6.3 -16 4
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 186304 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 186304 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 215616 None 0 Human Functional pEC50 = 6.3 6.3 -83 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
1334 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
71457994 78610 None 0 Mouse Functional pEC50 = 5.3 5.3 -12 3
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 78610 None 0 Mouse Functional pEC50 = 5.3 5.3 -12 3
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 205252 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 3
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 205252 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 3
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
155542149 173195 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 2
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 173195 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 2
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
155555182 174425 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 2
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 174425 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 2
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
155563222 175395 None 0 Mouse Functional pEC50 = 8.3 8.3 -16 3
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 175395 None 0 Mouse Functional pEC50 = 8.3 8.3 -16 3
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
118722929 116296 None 0 Mouse Functional pEC50 = 8.3 8.3 -6 3
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 116296 None 0 Mouse Functional pEC50 = 8.3 8.3 -6 3
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 213770 None 0 Mouse Functional pEC50 = 8.3 8.3 -1 4
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 None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL503449 216654 None 0 Mouse Functional pEC50 = 8.3 8.3 1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
118722925 116293 None 0 Mouse Functional pEC50 = 8.3 8.3 -7 3
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 116293 None 0 Mouse Functional pEC50 = 8.3 8.3 -7 3
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 121551 None 0 Mouse Functional pEC50 = 8.3 8.3 2 3
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 121551 None 0 Mouse Functional pEC50 = 8.3 8.3 2 3
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 181632 None 0 Mouse Functional pEC50 = 8.3 8.3 1 3
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 181632 None 0 Mouse Functional pEC50 = 8.3 8.3 1 3
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
1323 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.bmcl.2011.03.019
162649653 180206 None 0 Mouse Functional pEC50 = 8.2 8.2 -9 2
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 180206 None 0 Mouse Functional pEC50 = 8.2 8.2 -9 2
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
1323 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/ml500436s
92432 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/ml500436s
CHEMBL438294 216227 None 0 Human Functional pEC50 = 7.3 7.3 5 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155547310 173715 None 0 Mouse Functional pEC50 = 7.3 7.3 10 2
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 173715 None 0 Mouse Functional pEC50 = 7.3 7.3 10 2
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
155556954 174652 None 0 Mouse Functional pEC50 = 7.3 7.3 -165 3
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 174652 None 0 Mouse Functional pEC50 = 7.3 7.3 -165 3
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
155560756 175189 None 0 Mouse Functional pEC50 = 7.3 7.3 5 3
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 175189 None 0 Mouse Functional pEC50 = 7.3 7.3 5 3
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
132180599 156985 None 0 Mouse Functional pEC50 = 6.3 6.3 -2 3
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 156985 None 0 Mouse Functional pEC50 = 6.3 6.3 -2 3
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 184753 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 184753 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 159860 None 0 Mouse Functional pEC50 = 5.3 5.3 - 1
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 159860 None 0 Mouse Functional pEC50 = 5.3 5.3 - 1
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 211685 None 0 Human Functional pEC50 = 5.3 5.3 -14 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL455826 216480 None 0 Mouse Functional pEC50 = 7.3 7.3 1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL321870 213691 None 0 Mouse Functional pEC50 = 7.3 7.3 5 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
164627732 186600 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
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 186600 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
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 12279 None 0 Human Functional pEC50 = 6.3 6.3 -19 2
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 12279 None 0 Human Functional pEC50 = 6.3 6.3 -19 2
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
CHEMBL2145454 12279 None 0 Human Functional pEC50 = 6.3 6.3 -19 2
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
46885711 8072 None 0 Human Functional pEC50 = 5.3 5.3 -169 3
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 8072 None 0 Human Functional pEC50 = 5.3 5.3 -169 3
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 211970 None 0 Mouse Functional pEC50 = 7.3 7.3 -8 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
155568641 176201 None 0 Mouse Functional pEC50 = 7.3 7.3 -87 3
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 176201 None 0 Mouse Functional pEC50 = 7.3 7.3 -87 3
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 216055 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 3
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 None None None CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/acs.jmedchem.5b01894
137634090 156390 None 0 Mouse Functional pEC50 = 5.3 5.3 -3 5
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 156390 None 0 Mouse Functional pEC50 = 5.3 5.3 -3 5
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
44441647 154780 None 0 Human Functional pEC50 = 6.3 6.3 -22 3
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 154780 None 0 Human Functional pEC50 = 6.3 6.3 -22 3
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 184503 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
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 184503 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
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 185725 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 185725 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 32083 None 0 Mouse Functional pEC50 = 6.3 6.3 1 3
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 32083 None 0 Mouse Functional pEC50 = 6.3 6.3 1 3
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 16587 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 16587 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 32885 None 0 Mouse Functional pEC50 = 5.3 5.3 1 2
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 32885 None 0 Mouse Functional pEC50 = 5.3 5.3 1 2
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 185588 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 185588 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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
137657151 159650 None 0 Mouse Functional pEC50 = 5.3 5.3 -11 2
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 159650 None 0 Mouse Functional pEC50 = 5.3 5.3 -11 2
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 173909 None 0 Mouse Functional pEC50 = 7.3 7.3 7 3
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 173909 None 0 Mouse Functional pEC50 = 7.3 7.3 7 3
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 181577 None 0 Mouse Functional pEC50 = 6.3 6.3 -5 2
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 181577 None 0 Mouse Functional pEC50 = 6.3 6.3 -5 2
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
1334 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
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 None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
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 None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
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 None None None None 10.1021/jm049579s
CHEMBL410795 215302 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
1334 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
16133814 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.3 6.3 -17 4
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
137657206 159765 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 2
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 159765 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 2
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 215722 None 0 Mouse Functional pEC50 = 5.3 5.3 1 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL138212 211211 None 0 Mouse Functional pEC50 = 7.3 7.3 8 3
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O 10.1016/j.bmcl.2003.08.078
145966716 164400 None 0 Human Functional pEC50 = 6.3 6.3 -138 4
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 164400 None 0 Human Functional pEC50 = 6.3 6.3 -138 4
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 185235 None 0 Mouse Functional pEC50 = 6.3 6.3 12 3
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 185235 None 0 Mouse Functional pEC50 = 6.3 6.3 12 3
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 185847 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 185847 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
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 154391 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 154391 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 159434 None 0 Mouse Functional pEC50 = 6.2 6.2 -6 2
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 159434 None 0 Mouse Functional pEC50 = 6.2 6.2 -6 2
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 185250 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
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 185250 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
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 186697 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
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 186697 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
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
1323 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1016/j.ejmech.2018.04.021
172445559 195459 None 0 Human Functional pEC50 = 8.2 8.2 -4 4
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 195459 None 0 Human Functional pEC50 = 8.2 8.2 -4 4
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 211727 None 0 Human Functional pEC50 = 8.2 8.2 -64 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL195468 211561 None 0 Mouse Functional pEC50 = 8.2 8.2 -2 3
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
1323 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/acs.jmedchem.2c01587
92432 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/acs.jmedchem.2c01587
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.2 8.2 -181 7
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 None None None None 10.1021/acs.jmedchem.2c01587
16132144 211738 None 29 Mouse Functional pEC50 = 8.2 8.2 -1 8
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
16133793 211738 None 29 Mouse Functional pEC50 = 8.2 8.2 -1 8
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
44273719 211738 None 29 Mouse Functional pEC50 = 8.2 8.2 -1 8
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.2 8.2 -1 8
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
122184499 122459 None 0 Human Functional pEC50 = 7.2 7.2 -2 4
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 122459 None 0 Human Functional pEC50 = 7.2 7.2 -2 4
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 184533 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
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 184533 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
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 184825 None 0 Mouse Functional pEC50 = 6.2 6.2 47 3
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 184825 None 0 Mouse Functional pEC50 = 6.2 6.2 47 3
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 175757 None 0 Mouse Functional pEC50 = 6.2 6.2 -19 2
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 175757 None 0 Mouse Functional pEC50 = 6.2 6.2 -19 2
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 155996 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 2
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 155996 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 2
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
CHEMBL433296 216097 None 0 Mouse Functional pEC50 = 7.2 7.2 1 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
164622453 186196 None 0 Mouse Functional pEC50 = 6.2 6.2 2 3
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 186196 None 0 Mouse Functional pEC50 = 6.2 6.2 2 3
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
45487286 199797 None 0 Mouse Functional pEC50 = 5.2 5.2 -10 3
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 199797 None 0 Mouse Functional pEC50 = 5.2 5.2 -10 3
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 214285 None 0 Human Functional pEC50 = 7.2 7.2 2 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408276 75534 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
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 75534 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
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
45487298 199798 None 0 Mouse Functional pEC50 = 5.2 5.2 -7 3
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 199798 None 0 Mouse Functional pEC50 = 5.2 5.2 -7 3
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 211985 None 0 Mouse Functional pEC50 = 6.2 6.2 -39 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
164617159 185541 None 0 Mouse Functional pEC50 = 6.2 6.2 11 2
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 185541 None 0 Mouse Functional pEC50 = 6.2 6.2 11 2
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 94103 None 0 Human Functional pEC50 = 6.2 6.2 -11 2
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 94103 None 0 Human Functional pEC50 = 6.2 6.2 -11 2
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 210925 None 0 Mouse Functional pEC50 = 6.2 6.2 1 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
137662147 159473 None 0 Human Functional pEC50 = 6.2 6.2 -99 3
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 159473 None 0 Human Functional pEC50 = 6.2 6.2 -99 3
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
45487409 199353 None 0 Mouse Functional pEC50 = 5.2 5.2 -9 3
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 199353 None 0 Mouse Functional pEC50 = 5.2 5.2 -9 3
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 94583 None 0 Human Functional pEC50 = 6.2 6.2 -18 2
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 94583 None 0 Human Functional pEC50 = 6.2 6.2 -18 2
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 8042 None 0 Human Functional pEC50 = 5.2 5.2 -104 2
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 8042 None 0 Human Functional pEC50 = 5.2 5.2 -104 2
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
44408173 75427 None 0 Human Functional pEC50 = 6.2 6.2 -154 4
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 75427 None 0 Human Functional pEC50 = 6.2 6.2 -154 4
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 186057 None 0 Mouse Functional pEC50 = 6.2 6.2 72 2
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 186057 None 0 Mouse Functional pEC50 = 6.2 6.2 72 2
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 186609 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 186609 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 154494 None 0 Human Functional pEC50 = 6.2 6.2 -75 3
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 154494 None 0 Human Functional pEC50 = 6.2 6.2 -75 3
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 199697 None 0 Mouse Functional pEC50 = 5.2 5.2 -8 2
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 199697 None 0 Mouse Functional pEC50 = 5.2 5.2 -8 2
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 211910 None 0 Human Functional pEC50 = 6.2 6.2 1 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
137646086 157986 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 157986 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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
45487410 199894 None 0 Mouse Functional pEC50 = 5.2 5.2 -21 3
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 199894 None 0 Mouse Functional pEC50 = 5.2 5.2 -21 3
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 158172 None 0 Mouse Functional pEC50 = 6.2 6.2 -7 2
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 158172 None 0 Mouse Functional pEC50 = 6.2 6.2 -7 2
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 213685 None 0 Mouse Functional pEC50 = 6.2 6.2 1 3
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 None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
137641005 157131 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 157131 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 199557 None 0 Mouse Functional pEC50 = 5.2 5.2 -13 3
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 199557 None 0 Mouse Functional pEC50 = 5.2 5.2 -13 3
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 94180 None 0 Human Functional pEC50 = 6.2 6.2 -63 3
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 94180 None 0 Human Functional pEC50 = 6.2 6.2 -63 3
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 199350 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
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 199350 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
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 218350 None 0 Mouse Functional pEC50 = 5.2 5.2 1 3
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None 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 212730 None 0 Human Functional pEC50 = 7.2 7.2 -691 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O 10.1021/jm9017866
CHEMBL2323788 211973 None 0 Mouse Functional pEC50 = 6.2 6.2 -13 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
45487414 199737 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
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 199737 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
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 158242 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 158242 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 213694 None 0 Mouse Functional pEC50 = 5.2 5.2 3 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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 214272 None 0 Human Functional pEC50 = 8.2 8.2 -2 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
15602927 157974 None 0 Mouse Functional pEC50 = 8.2 8.2 -1 4
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 157974 None 0 Mouse Functional pEC50 = 8.2 8.2 -1 4
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 213693 None 0 Mouse Functional pEC50 = 8.1 8.1 2 4
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL501394 216625 None 0 Mouse Functional pEC50 = 8.1 8.1 -2 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
162672755 183196 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 2
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 183196 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 2
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 216607 None 1 Mouse Functional pEC50 = 7.2 7.2 -8 6
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 None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
137658252 159723 None 0 Mouse Functional pEC50 = 7.2 7.2 6 3
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 159723 None 0 Mouse Functional pEC50 = 7.2 7.2 6 3
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 199236 None 0 Mouse Functional pEC50 = 4.2 4.2 -22 3
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 199236 None 0 Mouse Functional pEC50 = 4.2 4.2 -22 3
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
44401520 13935 None 0 Human Functional pEC50 = 6.2 6.2 -181 2
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 13935 None 0 Human Functional pEC50 = 6.2 6.2 -181 2
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
CHEMBL557154 13935 None 0 Human Functional pEC50 = 6.2 6.2 -181 2
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 159470 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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 159470 None 0 Mouse Functional pEC50 = 4.2 4.2 - 1
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
51351151 58822 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 3
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 58822 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 3
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 58822 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 3
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 58822 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 3
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 156370 None 0 Mouse Functional pEC50 = 4.1 4.1 - 1
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 156370 None 0 Mouse Functional pEC50 = 4.1 4.1 - 1
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
145948912 167583 None 0 Human Functional pEC50 = 7.1 7.1 -2 4
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 167583 None 0 Human Functional pEC50 = 7.1 7.1 -2 4
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 121550 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 3
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 121550 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 3
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 212327 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL105113 210925 None 0 Mouse Functional pEC50 = 6.1 6.1 1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1338 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 3807 None 36 Human Functional pEC50 = 6.1 6.1 -660 8
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 31487 None 0 Mouse Functional pEC50 = 5.1 5.1 3 3
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 31487 None 0 Mouse Functional pEC50 = 5.1 5.1 3 3
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
CHEMBL438235 216220 None 0 Human Functional pEC50 = 7.1 7.1 -3 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
164621414 185880 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
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 185880 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
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 210922 None 0 Mouse Functional pEC50 = 5.1 5.1 2 2
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
155562846 175274 None 0 Mouse Functional pEC50 = 5.1 5.1 -6 2
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 175274 None 0 Mouse Functional pEC50 = 5.1 5.1 -6 2
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
137656521 159838 None 0 Human Functional pEC50 = 6.1 6.1 -33 3
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 159838 None 0 Human Functional pEC50 = 6.1 6.1 -33 3
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
44401524 14011 None 0 Human Functional pEC50 = 6.1 6.1 -120 2
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 14011 None 0 Human Functional pEC50 = 6.1 6.1 -120 2
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
CHEMBL559181 14011 None 0 Human Functional pEC50 = 6.1 6.1 -120 2
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
CHEMBL227833 211911 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2323792 211977 None 0 Mouse Functional pEC50 = 5.1 5.1 1 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
127047336 139885 None 0 Mouse Functional pEC50 = 6.1 6.1 -74 3
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 139885 None 0 Mouse Functional pEC50 = 6.1 6.1 -74 3
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 130387 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
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 130387 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
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
1323 2688 None 38 Human Functional pEC50 = 8.1 8.1 -181 7
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 None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 38 Human Functional pEC50 = 8.1 8.1 -181 7
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 None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.1 8.1 -181 7
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 None None None None 10.1016/j.bmcl.2006.07.015
155556466 174520 None 0 Mouse Functional pEC50 = 8.1 8.1 -11 3
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 174520 None 0 Mouse Functional pEC50 = 8.1 8.1 -11 3
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 216631 None 0 Mouse Functional pEC50 = 8.1 8.1 1 3
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
46232226 203540 None 0 Mouse Functional pEC50 = 8.1 8.1 6 3
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 203540 None 0 Mouse Functional pEC50 = 8.1 8.1 6 3
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 218289 None 0 Mouse Functional pEC50 = 8.1 8.1 1 3
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 None None None 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
16132144 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16133793 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
44273719 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16132144 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
16133793 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44273719 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.1 8.1 -81 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL415200 215639 None 0 Mouse Functional pEC50 = 8.1 8.1 5 5
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
132180598 157941 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 3
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 157941 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 3
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
155562237 175813 None 0 Mouse Functional pEC50 = 7.1 7.1 -39 3
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 175813 None 0 Mouse Functional pEC50 = 7.1 7.1 -39 3
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 140640 None 0 Human Functional pEC50 = 6.1 6.1 -114 4
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 140640 None 0 Human Functional pEC50 = 6.1 6.1 -114 4
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
164622957 186220 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 186220 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 186670 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 186670 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 213864 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
122184912 122624 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 122624 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 214704 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
16157270 215013 None 15 Human Functional pEC50 = 7.1 7.1 -109 6
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 215013 None 15 Human Functional pEC50 = 7.1 7.1 -109 6
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL411359 215339 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
16157270 215013 None 15 Human Functional pEC50 = 7.1 7.1 -109 6
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 215013 None 15 Human Functional pEC50 = 7.1 7.1 -109 6
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
155551195 174046 None 0 Mouse Functional pEC50 = 6.1 6.1 -38 3
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 174046 None 0 Mouse Functional pEC50 = 6.1 6.1 -38 3
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 102816 None 0 Mouse Functional pEC50 = 5.1 5.1 -2 3
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 102816 None 0 Mouse Functional pEC50 = 5.1 5.1 -2 3
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 205797 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
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 205797 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
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 211972 None 0 Mouse Functional pEC50 = 6.1 6.1 -41 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137635701 156128 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 3
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 156128 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 3
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 214284 None 0 Human Functional pEC50 = 6.1 6.1 -6 4
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44391929 12416 None 0 Human Functional pEC50 = 6.1 6.1 -25 2
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 12416 None 0 Human Functional pEC50 = 6.1 6.1 -25 2
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
CHEMBL2145453 12416 None 0 Human Functional pEC50 = 6.1 6.1 -25 2
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 216640 None 0 Human Functional pEC50 = 7.1 7.1 -6 4
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL381739 214752 None 0 Human Functional pEC50 = 6.1 6.1 4 3
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
44408154 141449 None 0 Human Functional pEC50 = 6.1 6.1 -218 4
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 141449 None 0 Human Functional pEC50 = 6.1 6.1 -218 4
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 211982 None 0 Mouse Functional pEC50 = 6.1 6.1 -44 3
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 None None None C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm301253y
1337 3424 None 5 Human Functional pEC50 = 6.1 6.1 -3 5
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 3424 None 5 Human Functional pEC50 = 6.1 6.1 -3 5
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 3424 None 5 Human Functional pEC50 = 6.1 6.1 -3 5
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 126849 None 0 Human Functional pEC50 = 6.1 6.1 -34 3
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 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL365401 126849 None 0 Human Functional pEC50 = 6.1 6.1 -34 3
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 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
45487292 199308 None 0 Mouse Functional pEC50 = 5.1 5.1 -4 3
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 199308 None 0 Mouse Functional pEC50 = 5.1 5.1 -4 3
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 211981 None 0 Mouse Functional pEC50 = 7.1 7.1 -79 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
24882615 97545 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 3
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 97545 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 3
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 213820 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
CHEMBL408509 215180 None 0 Human Functional pEC50 = 6.1 6.1 2 3
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44401310 12789 None 0 Human Functional pEC50 = 6.1 6.1 -125 2
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 12789 None 0 Human Functional pEC50 = 6.1 6.1 -125 2
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
CHEMBL534930 12789 None 0 Human Functional pEC50 = 6.1 6.1 -125 2
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
71456219 78778 None 0 Human Functional pEC50 = 6.1 6.1 -23 3
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 78778 None 0 Human Functional pEC50 = 6.1 6.1 -23 3
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 94184 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 94184 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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
162672755 183196 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 2
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 183196 None 0 Mouse Functional pEC50 = 8.1 8.1 -16 2
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 211980 None 0 Mouse Functional pEC50 = 8.0 8.0 -19 3
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.0 8.0 2 7
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL2369485 212087 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 3
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
155549302 173907 None 0 Mouse Functional pEC50 = 7.1 7.1 1 2
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 173907 None 0 Mouse Functional pEC50 = 7.1 7.1 1 2
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
155554827 174723 None 0 Mouse Functional pEC50 = 5.1 5.1 -2 2
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 174723 None 0 Mouse Functional pEC50 = 5.1 5.1 -2 2
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 175335 None 0 Mouse Functional pEC50 = 5.1 5.1 1 2
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 175335 None 0 Mouse Functional pEC50 = 5.1 5.1 1 2
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 156015 None 0 Human Functional pEC50 = 6.0 6.0 -162 3
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 156015 None 0 Human Functional pEC50 = 6.0 6.0 -162 3
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 11800 None 0 Human Functional pEC50 = 6.0 6.0 -19 2
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 11800 None 0 Human Functional pEC50 = 6.0 6.0 -19 2
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
CHEMBL2028960 11800 None 0 Human Functional pEC50 = 6.0 6.0 -19 2
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 58823 None 0 Mouse Functional pEC50 = 6.0 6.0 -5 3
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 58823 None 0 Mouse Functional pEC50 = 6.0 6.0 -5 3
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 58823 None 0 Mouse Functional pEC50 = 6.0 6.0 -5 3
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 58823 None 0 Mouse Functional pEC50 = 6.0 6.0 -5 3
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 58823 None 0 Mouse Functional pEC50 = 6.0 6.0 -5 3
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 199895 None 0 Mouse Functional pEC50 = 6.0 6.0 -11 3
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 199895 None 0 Mouse Functional pEC50 = 6.0 6.0 -11 3
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 186073 None 0 Mouse Functional pEC50 = 6.0 6.0 2 2
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 186073 None 0 Mouse Functional pEC50 = 6.0 6.0 2 2
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 164752 None 0 Human Functional pEC50 = 7.0 7.0 -22 4
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 164752 None 0 Human Functional pEC50 = 7.0 7.0 -22 4
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 7756 None 0 Human Functional pEC50 = 6.0 6.0 -63 3
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 7756 None 0 Human Functional pEC50 = 6.0 6.0 -63 3
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 199279 None 0 Mouse Functional pEC50 = 5.0 5.0 -8 2
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 199279 None 0 Mouse Functional pEC50 = 5.0 5.0 -8 2
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
CHEMBL430489 216081 None 0 Mouse Functional pEC50 = 5.0 5.0 2 3
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None 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
44441681 94182 None 0 Human Functional pEC50 = 6.0 6.0 -104 2
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 94182 None 0 Human Functional pEC50 = 6.0 6.0 -104 2
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 216309 None 0 Human Functional pEC50 = 7 7.0 -16 3
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438030 216205 None 0 Human Functional pEC50 = 7 7.0 -63 3
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
51351024 58819 None 0 Mouse Functional pEC50 = 6 6.0 -4 3
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 58819 None 0 Mouse Functional pEC50 = 6 6.0 -4 3
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 58819 None 0 Mouse Functional pEC50 = 6 6.0 -4 3
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 58819 None 0 Mouse Functional pEC50 = 6 6.0 -4 3
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
168277916 190786 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 190786 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 192006 None 0 Human Functional pIC50 = 5.0 5.0 -1288 4
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 192006 None 0 Human Functional pIC50 = 5.0 5.0 -1288 4
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 192275 None 0 Human Functional pIC50 = 6.9 6.9 -1288 4
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 192275 None 0 Human Functional pIC50 = 6.9 6.9 -1288 4
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 191224 None 0 Human Functional pIC50 = 5.9 5.9 -2818 4
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 191224 None 0 Human Functional pIC50 = 5.9 5.9 -2818 4
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 190374 None 0 Human Functional pIC50 = 6.9 6.9 -1584 4
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 190374 None 0 Human Functional pIC50 = 6.9 6.9 -1584 4
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 191753 None 0 Human Functional pIC50 = 4.8 4.8 -7079 4
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 191753 None 0 Human Functional pIC50 = 4.8 4.8 -7079 4
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 190434 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 190434 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 190597 None 0 Human Functional pIC50 = 5.8 5.8 -6760 4
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 190597 None 0 Human Functional pIC50 = 5.8 5.8 -6760 4
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 191779 None 0 Human Functional pIC50 = 4.8 4.8 -10232 4
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 191779 None 0 Human Functional pIC50 = 4.8 4.8 -10232 4
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 192299 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 192299 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 190372 None 0 Human Functional pIC50 = 4.8 4.8 -6025 4
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 190372 None 0 Human Functional pIC50 = 4.8 4.8 -6025 4
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 191348 None 0 Human Functional pIC50 = 6.7 6.7 -331 4
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 191348 None 0 Human Functional pIC50 = 6.7 6.7 -331 4
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 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 20 Human Functional pIC50 = 5.7 5.7 -12589 5
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 None None None None 10.1021/acs.jmedchem.2c00793
168272660 190542 None 0 Human Functional pIC50 = 6.7 6.7 -1548 4
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 190542 None 0 Human Functional pIC50 = 6.7 6.7 -1548 4
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 190784 None 0 Human Functional pIC50 = 4.7 4.7 -4897 4
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 190784 None 0 Human Functional pIC50 = 4.7 4.7 -4897 4
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 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 23 Human Functional pIC50 = 6.7 6.7 -467 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
168289457 191489 None 0 Human Functional pIC50 = 6.7 6.7 -1047 4
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 191489 None 0 Human Functional pIC50 = 6.7 6.7 -1047 4
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 190496 None 0 Human Functional pIC50 = 4.7 4.7 -4073 4
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 190496 None 0 Human Functional pIC50 = 4.7 4.7 -4073 4
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 191055 None 0 Human Functional pIC50 = 6.7 6.7 -4570 4
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 191055 None 0 Human Functional pIC50 = 6.7 6.7 -4570 4
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 190194 None 0 Human Functional pIC50 = 7.6 7.6 -288 4
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 190194 None 0 Human Functional pIC50 = 7.6 7.6 -288 4
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 192584 None 0 Human Functional pIC50 = 4.6 4.6 -13489 4
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 192584 None 0 Human Functional pIC50 = 4.6 4.6 -13489 4
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 190064 None 0 Human Functional pIC50 = 6.6 6.6 -1819 4
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 190064 None 0 Human Functional pIC50 = 6.6 6.6 -1819 4
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
1323 2688 None 38 Human Functional pIC50 = 7.6 7.6 -181 7
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 None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 38 Human Functional pIC50 = 7.6 7.6 -181 7
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 None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 38 Human Functional pIC50 = 7.6 7.6 -181 7
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 None None None None 10.1021/acs.jmedchem.2c00793
168276294 190617 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 190617 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 191733 None 0 Human Functional pIC50 = 7.4 7.4 -162 4
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 191733 None 0 Human Functional pIC50 = 7.4 7.4 -162 4
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 191421 None 0 Human Functional pIC50 = 7.4 7.4 -933 4
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 191421 None 0 Human Functional pIC50 = 7.4 7.4 -933 4
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 190819 None 0 Human Functional pIC50 = 5.4 5.4 -870 4
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 190819 None 0 Human Functional pIC50 = 5.4 5.4 -870 4
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 191031 None 0 Human Functional pIC50 = 7.2 7.2 -218 4
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 191031 None 0 Human Functional pIC50 = 7.2 7.2 -218 4
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 190409 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 190409 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 192514 None 0 Human Functional pIC50 = 6.1 6.1 -9120 4
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 192514 None 0 Human Functional pIC50 = 6.1 6.1 -9120 4
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 191066 None 0 Human Functional pIC50 = 7.1 7.1 -794 3
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 191066 None 0 Human Functional pIC50 = 7.1 7.1 -794 3
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 215535 None 0 Human Functional pKd = 8.7 8.7 -1 4
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
44445085 97127 None 0 Human Functional pKd = 8.7 8.7 -1 4
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 97127 None 0 Human Functional pKd = 8.7 8.7 -1 4
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 195544 None 0 Mouse Functional pKd = 6 6.0 - 0
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 195544 None 0 Mouse Functional pKd = 6 6.0 - 0
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
164620129 185853 None 0 Mouse Functional pKd = 5.9 5.9 - 0
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 185853 None 0 Mouse Functional pKd = 5.9 5.9 - 0
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 196162 None 0 Mouse Functional pKd = 5.9 5.9 - 1
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 196162 None 0 Mouse Functional pKd = 5.9 5.9 - 1
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
172451922 195576 None 0 Mouse Functional pKd = 5.8 5.8 - 0
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 195576 None 0 Mouse Functional pKd = 5.8 5.8 - 0
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 195435 None 0 Mouse Functional pKd = 6.7 6.7 - 1
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 195435 None 0 Mouse Functional pKd = 6.7 6.7 - 1
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 195668 None 0 Mouse Functional pKd = 6.7 6.7 - 0
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 195668 None 0 Mouse Functional pKd = 6.7 6.7 - 0
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 195165 None 0 Mouse Functional pKd = 5.7 5.7 - 0
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 195165 None 0 Mouse Functional pKd = 5.7 5.7 - 0
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
164619641 185832 None 0 Mouse Functional pKd = 6.6 6.6 - 0
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 185832 None 0 Mouse Functional pKd = 6.6 6.6 - 0
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
132938008 159607 None 0 Mouse Functional pKd = 7.5 7.5 -891 4
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@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4102048 159607 None 0 Mouse Functional pKd = 7.5 7.5 -891 4
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@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
155561116 175077 None 0 Mouse Functional pKd = 6.5 6.5 -269 4
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 175077 None 0 Mouse Functional pKd = 6.5 6.5 -269 4
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 122500 None 0 Human Functional pKd = 7.4 7.4 2 4
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 122500 None 0 Human Functional pKd = 7.4 7.4 2 4
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 180177 None 0 Mouse Functional pKd = 7.4 7.4 - 1
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 180177 None 0 Mouse Functional pKd = 7.4 7.4 - 1
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 214209 None 1 Mouse Functional pKd = 6.4 6.4 -177 4
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
171378453 196322 None 0 Mouse Functional pKd = 6.4 6.4 - 1
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 196322 None 0 Mouse Functional pKd = 6.4 6.4 - 1
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 214209 None 1 Mouse Functional pKd = 6.4 6.4 -177 4
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
44577515 189115 None 0 Human Functional pKd = 8.3 8.3 -2 2
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 189115 None 0 Human Functional pKd = 8.3 8.3 -2 2
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
132938008 159607 None 0 Mouse Functional pKd = 7.3 7.3 -891 4
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@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4102048 159607 None 0 Mouse Functional pKd = 7.3 7.3 -891 4
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@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
172452729 195923 None 0 Mouse Functional pKd = 6.3 6.3 - 0
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 195923 None 0 Mouse Functional pKd = 6.3 6.3 - 0
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
172456626 196231 None 0 Mouse Functional pKd = 6.3 6.3 - 0
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 196231 None 0 Mouse Functional pKd = 6.3 6.3 - 0
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
155544852 175043 None 0 Mouse Functional pKd = 6.3 6.3 -331 4
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 175043 None 0 Mouse Functional pKd = 6.3 6.3 -331 4
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 195068 None 0 Mouse Functional pKd = 7.2 7.2 - 0
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 195068 None 0 Mouse Functional pKd = 7.2 7.2 - 0
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 179556 None 0 Mouse Functional pKd = 6.1 6.1 - 1
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 179556 None 0 Mouse Functional pKd = 6.1 6.1 - 1
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
172449003 195928 None 0 Mouse Functional pKd = 6.1 6.1 - 0
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 195928 None 0 Mouse Functional pKd = 6.1 6.1 - 0
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
172449408 195948 None 0 Mouse Functional pKd = 6.1 6.1 - 0
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 195948 None 0 Mouse Functional pKd = 6.1 6.1 - 0
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
155548853 173913 None 0 Mouse Functional pKd = 6.1 6.1 -758 4
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 173913 None 0 Mouse Functional pKd = 6.1 6.1 -758 4
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
131839615 215096 None 23 Mouse Functional pEC50 = 8.0 8.0 -1 6
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
16133835 215096 None 23 Mouse Functional pEC50 = 8.0 8.0 -1 6
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
CHEMBL407070 215096 None 23 Mouse Functional pEC50 = 8.0 8.0 -1 6
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
131839615 215096 None 23 Human Functional pIC50 = 8.1 8.1 1 6
NoneNone
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
16133835 215096 None 23 Human Functional pIC50 = 8.1 8.1 1 6
NoneNone
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
CHEMBL407070 215096 None 23 Human Functional pIC50 = 8.1 8.1 1 6
NoneNone
Drug Central None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C None
1341 3076 None 0 Human Functional pIC50 None 10.5 10.5 6 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1335 315 None 0 Human Functional pIC50 None 6.5 6.5 -630 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9892020
1342 247 None 0 Human Functional pIC50 None 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12904077
1324 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16154396 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16197727 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16197727.0 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
44285019 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
57514683 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
91898441 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL441738 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
DB04931 302 None 19 Human Functional pIC50 None 9 9.0 -13 8
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1323 2688 None 38 Human Functional pIC50 None 9 9.0 -181 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
92432 2688 None 38 Human Functional pIC50 None 9 9.0 -181 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL430239 2688 None 38 Human Functional pIC50 None 9 9.0 -181 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

44366081 10264 None 0 Human Binding pEC50 = 10.5 10.5 - 2
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 10264 None 0 Human Binding pEC50 = 10.5 10.5 - 2
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
1323 2688 None 38 Mouse Binding pEC50 = 10.2 10.2 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
92432 2688 None 38 Mouse Binding pEC50 = 10.2 10.2 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL430239 2688 None 38 Mouse Binding pEC50 = 10.2 10.2 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16154396 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727.0 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44285019 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
57514683 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
91898441 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL441738 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
DB04931 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
1324 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
16154396 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727.0 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
44285019 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
57514683 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
91898441 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
CHEMBL441738 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
DB04931 302 None 19 Mouse Binding pEC50 = 10.2 10.2 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
101176453 183068 None 0 Human Binding pEC50 = 10.1 10.1 - 0
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 183068 None 0 Human Binding pEC50 = 10.1 10.1 - 0
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 210967 None 0 Human Binding pEC50 = 10.1 10.1 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
1324 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
16154396 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727.0 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
44285019 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
57514683 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
91898441 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL441738 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
DB04931 302 None 19 Mouse Binding pEC50 = 10.0 10.0 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL2096742 211665 None 0 Human Binding pEC50 = 9.9 9.9 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
CHEMBL442504 216377 None 0 Human Binding pEC50 = 9.9 9.9 -1 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
1323 2688 None 38 Mouse Binding pEC50 = 9.8 9.8 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
92432 2688 None 38 Mouse Binding pEC50 = 9.8 9.8 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL430239 2688 None 38 Mouse Binding pEC50 = 9.8 9.8 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44327392 141950 None 0 Mouse Binding pEC50 = 9.8 9.8 - 0
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 141950 None 0 Mouse Binding pEC50 = 9.8 9.8 - 0
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 210968 None 0 Human Binding pEC50 = 9.7 9.7 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
16132144 211738 None 29 Mouse Binding pEC50 = 9.5 9.5 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049010r
16133793 211738 None 29 Mouse Binding pEC50 = 9.5 9.5 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049010r
44273719 211738 None 29 Mouse Binding pEC50 = 9.5 9.5 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049010r
CHEMBL214332 211738 None 29 Mouse Binding pEC50 = 9.5 9.5 - 4
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049010r
CHEMBL2369959 212199 None 0 Mouse Binding pEC50 = 9.4 9.4 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
16132144 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm020296e
16133793 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm020296e
44273719 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm020296e
CHEMBL214332 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm020296e
16132144 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0104872
16133793 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0104872
44273719 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0104872
CHEMBL214332 211738 None 29 Mouse Binding pEC50 = 9.4 9.4 - 4
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0104872
CHEMBL2369967 212207 None 0 Mouse Binding pEC50 = 9.3 9.3 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
1323 2688 None 38 Mouse Binding pEC50 = 9.2 9.2 - 4
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 None None None None 10.1021/ml500340z
92432 2688 None 38 Mouse Binding pEC50 = 9.2 9.2 - 4
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 None None None None 10.1021/ml500340z
CHEMBL430239 2688 None 38 Mouse Binding pEC50 = 9.2 9.2 - 4
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 None None None None 10.1021/ml500340z
CHEMBL2369964 212204 None 0 Mouse Binding pEC50 = 9.0 9.0 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44322868 106064 None 0 Human Binding pEC50 = 9 9.0 -4 3
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 106064 None 0 Human Binding pEC50 = 9 9.0 -4 3
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 212203 None 0 Mouse Binding pEC50 = 8.7 8.7 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL1161318 210964 None 0 Human Binding pEC50 = 8 8.0 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
CHEMBL347364 214172 None 0 Mouse Binding pEC50 = 7 7.0 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
CHEMBL191063 211538 None 0 Mouse Binding pEC50 = 7 7.0 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL365794 214501 None 0 Mouse Binding pEC50 = 6 6.0 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
11038873 171983 None 0 Human Binding pEC50 = 5 5.0 - 0
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 171983 None 0 Human Binding pEC50 = 5 5.0 - 0
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 168306 None 0 Human Binding pEC50 = 6.0 6.0 -6 3
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 168306 None 0 Human Binding pEC50 = 6.0 6.0 -6 3
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 214171 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
CHEMBL190080 211521 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL275303 213280 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL432027 216092 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
46877881 204275 None 0 Human Binding pEC50 = 5.9 5.9 -5 3
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 204275 None 0 Human Binding pEC50 = 5.9 5.9 -5 3
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 218399 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL327479 213753 None 0 Mouse Binding pEC50 = 6.8 6.8 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL433522 216102 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccncc1)C(N)=O 10.1021/jm020296e
CHEMBL190551 211525 None 0 Mouse Binding pEC50 = 7.8 7.8 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL348901 214175 None 0 Mouse Binding pEC50 = 6.8 6.8 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
44323234 168159 None 0 Human Binding pEC50 = 6.8 6.8 -11 3
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 168159 None 0 Human Binding pEC50 = 6.8 6.8 -11 3
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 210966 None 0 Human Binding pEC50 = 7.8 7.8 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
CHEMBL2371147 212476 None 0 Mouse Binding pEC50 = 6.8 6.8 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
CHEMBL3422431 214129 None 0 Mouse Binding pEC50 = 5.8 5.8 - 1
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 None None None 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
118735610 118945 None 0 Mouse Binding pEC50 = 4.7 4.7 - 1
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 118945 None 0 Mouse Binding pEC50 = 4.7 4.7 - 1
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 211536 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL372237 214632 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2372589 212732 None 0 Human Binding pEC50 = 8.7 8.7 - 2
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
171355776 194266 None 0 Human Binding pEC50 = 8.7 8.7 - 0
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 194266 None 0 Human Binding pEC50 = 8.7 8.7 - 0
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 212209 None 0 Mouse Binding pEC50 = 8.7 8.7 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2096742 211665 None 0 Mouse Binding pEC50 = 8.6 8.6 - 2
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm049010r
CHEMBL2369973 212213 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(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
1325 3600 None 12 Mouse Binding pEC50 = 8.6 8.6 - 6
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 None None None None 10.1021/ml500340z
6440621 3600 None 12 Mouse Binding pEC50 = 8.6 8.6 - 6
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 None None None None 10.1021/ml500340z
9898183 3600 None 12 Mouse Binding pEC50 = 8.6 8.6 - 6
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 None None None None 10.1021/ml500340z
CHEMBL3422426 3600 None 12 Mouse Binding pEC50 = 8.6 8.6 - 6
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 None None None None 10.1021/ml500340z
118735609 118944 None 0 Mouse Binding pEC50 = 4.7 4.7 - 1
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 118944 None 0 Mouse Binding pEC50 = 4.7 4.7 - 1
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 30268 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 30268 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 212214 None 0 Mouse Binding pEC50 = 7.7 7.7 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](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 213776 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
118735606 118943 None 0 Mouse Binding pEC50 = 4.6 4.6 - 1
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 118943 None 0 Mouse Binding pEC50 = 4.6 4.6 - 1
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 210332 None 0 Mouse Binding pEC50 = 5.6 5.6 - 0
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 210332 None 0 Mouse Binding pEC50 = 5.6 5.6 - 0
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 211666 None 0 Mouse Binding pEC50 = 4.6 4.6 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/jm020296e
CHEMBL191120 211539 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL370321 214627 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44269214 98547 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 98547 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 118941 None 0 Mouse Binding pEC50 = 5.6 5.6 - 1
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 118941 None 0 Mouse Binding pEC50 = 5.6 5.6 - 1
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 213780 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2369982 212222 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369960 212200 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](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 212260 None 0 Human Binding pEC50 = 8.5 8.5 -6 3
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
CHEMBL2369965 212205 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44369234 45260 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 45260 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 213067 None 0 Mouse Binding pEC50 = 8.4 8.4 - 1
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL330233 213790 None 0 Mouse Binding pEC50 = 6.5 6.5 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL365913 214503 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL188738 211518 None 0 Mouse Binding pEC50 = 6.5 6.5 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL189991 211520 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2369976 212216 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL154153 211259 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL264190 213067 None 0 Mouse Binding pEC50 = 7.5 7.5 - 1
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL350012 214181 None 0 Mouse Binding pEC50 = 4.4 4.4 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm020296e
CHEMBL96871 218411 None 0 Mouse Binding pEC50 = 6.4 6.4 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL431092 216083 None 0 Mouse Binding pEC50 = 6.4 6.4 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2371150 212477 None 0 Mouse Binding pEC50 = 4.4 4.4 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm020296e
CHEMBL1161320 210965 None 0 Human Binding pEC50 = 6.4 6.4 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
44269189 98391 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 98391 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 211523 None 0 Mouse Binding pEC50 = 5.4 5.4 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL264190 213067 None 0 Mouse Binding pEC50 = 8.3 8.3 - 1
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL357558 214203 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
CHEMBL2369983 212223 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL330561 213792 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1cccs1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL317969 213667 None 0 Mouse Binding pEC50 = 6.4 6.4 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None 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 162018 None 0 Human Binding pEC50 = 7.4 7.4 -208 3
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 162018 None 0 Human Binding pEC50 = 7.4 7.4 -208 3
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 162018 None 0 Human Binding pEC50 = 7.4 7.4 -208 3
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 212206 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369961 212201 None 0 Mouse Binding pEC50 = 6.4 6.4 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)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
9915813 38500 None 15 Human Binding pEC50 = 5.4 5.4 - 0
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 38500 None 15 Human Binding pEC50 = 5.4 5.4 - 0
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 210963 None 0 Human Binding pEC50 = 7.4 7.4 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
10101361 155793 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 155793 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 211253 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL154251 211260 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL2369975 212215 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369970 212210 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2371832 212594 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL432201 216094 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
44366171 121358 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 121358 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 214128 None 0 Mouse Binding pEC50 = 5.3 5.3 - 1
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 None None None 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 209384 None 0 Human Binding pEC50 = 6.3 6.3 -114 3
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 209384 None 0 Human Binding pEC50 = 6.3 6.3 -114 3
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 218398 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2371835 212596 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL186970 211513 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2371829 212593 None 0 Mouse Binding pEC50 = 5.2 5.2 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL2371833 212595 None 0 Mouse Binding pEC50 = 5.2 5.2 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
44323020 169099 None 0 Human Binding pEC50 = 6.2 6.2 -741 3
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 169099 None 0 Human Binding pEC50 = 6.2 6.2 -741 3
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 213685 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2369968 212208 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None 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 212211 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]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 211663 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/jm020296e
CHEMBL2369962 212202 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL152555 211254 None 0 Mouse Binding pEC50 = 5.2 5.2 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL358833 214263 None 0 Mouse Binding pEC50 = 5.1 5.1 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL346925 214170 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
118735605 118942 None 0 Mouse Binding pEC50 = 5.1 5.1 - 1
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 118942 None 0 Mouse Binding pEC50 = 5.1 5.1 - 1
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 212212 None 0 Mouse Binding pEC50 = 5.1 5.1 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL373344 214635 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL188459 211516 None 0 Mouse Binding pEC50 = 5.1 5.1 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190102 211522 None 0 Mouse Binding pEC50 = 5.1 5.1 - 0
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)Cc1ccccc1 10.1021/jm0490033
CHEMBL2369977 212217 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL349795 214179 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccs1)C(N)=O 10.1021/jm020296e
CHEMBL152986 211256 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL317968 213666 None 0 Mouse Binding pEC50 = 7.0 7.0 - 0
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
11813437 98582 None 0 Human Binding pEC50 = 5.0 5.0 - 0
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 98582 None 0 Human Binding pEC50 = 5.0 5.0 - 0
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 212476 None 0 Mouse Binding pEC50 = 6.0 6.0 - 0
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
44366081 10264 None 0 Human Binding pIC50 = 10.6 10.6 - 2
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 10264 None 0 Human Binding pIC50 = 10.6 10.6 - 2
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 210967 None 0 Human Binding pIC50 = 10.5 10.5 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 211665 None 0 Human Binding pIC50 = 10.1 10.1 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
16049796 83499 None 0 Human Binding pIC50 = 10 10.0 - 0
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 83499 None 0 Human Binding pIC50 = 10 10.0 - 0
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 166105 None 0 Human Binding pIC50 = 10 10.0 - 0
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 166105 None 0 Human Binding pIC50 = 10 10.0 - 0
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 210968 None 0 Human Binding pIC50 = 10.0 10.0 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL2371966 212622 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
44418413 83245 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 83245 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 83207 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 83207 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 216629 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2371962 212618 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
44418420 142034 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 142034 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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
1324 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
1324 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
1324 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 19 Human Binding pIC50 = 9.1 9.1 -6 4
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL2096742 211665 None 0 Human Binding pIC50 = 9.1 9.1 - 2
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm801300c
CHEMBL2371968 212624 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL524861 218113 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2372589 212732 None 0 Human Binding pIC50 = 8.9 8.9 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL204310 211623 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0510326
1323 2688 None 38 Human Binding pIC50 = 8.8 8.8 -346 4
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 None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 38 Human Binding pIC50 = 8.8 8.8 -346 4
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 None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.8 8.8 -346 4
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 None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL2371965 212621 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
71449048 78512 None 0 Human Binding pIC50 = 8 8.0 - 0
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 78512 None 0 Human Binding pIC50 = 8 8.0 - 0
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 211620 None 0 Human Binding pIC50 = 8 8.0 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0510326
CHEMBL446185 216405 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
CHEMBL1775062 211339 None 0 Human Binding pIC50 = 6 6.0 - 0
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 None None None C[C@@H]1NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
137659790 159416 None 0 Human Binding pIC50 = 6 6.0 - 3
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 159416 None 0 Human Binding pIC50 = 6 6.0 - 3
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 211525 None 0 Mouse Binding pIC50 = 6 6.0 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL408509 215180 None 0 Human Binding pIC50 = 6 6.0 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL5077811 217004 None 0 Human Binding pIC50 = 5 5.0 - 3
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 None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL372237 214632 None 0 Mouse Binding pIC50 = 5 5.0 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
44396987 67214 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 67214 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 122624 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 122624 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 167400 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 167400 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 213067 None 0 Human Binding pIC50 = 7.0 7.0 - 1
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL264190 213067 None 0 Human Binding pIC50 = 7.0 7.0 - 1
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 None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.2c01794
CHEMBL2096759 211667 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44408287 75412 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 75412 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 215813 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
49862378 15048 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 15048 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 79005 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 79005 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 158054 None 0 Human Binding pIC50 = 6.0 6.0 - 3
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 158054 None 0 Human Binding pIC50 = 6.0 6.0 - 3
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 157636 None 0 Human Binding pIC50 = 5.0 5.0 - 3
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 157636 None 0 Human Binding pIC50 = 5.0 5.0 - 3
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 217492 None 0 Human Binding pIC50 = 5.0 5.0 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL3601426 214286 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
16132144 211738 None 29 Human Binding pIC50 = 6.9 6.9 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
16133793 211738 None 29 Human Binding pIC50 = 6.9 6.9 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44273719 211738 None 29 Human Binding pIC50 = 6.9 6.9 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL214332 211738 None 29 Human Binding pIC50 = 6.9 6.9 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL1161321 210966 None 0 Human Binding pIC50 = 7.9 7.9 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
145976444 164058 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 164058 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 154347 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 154347 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 123701 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 123701 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 173634 None 0 Mouse Binding pIC50 = 4.9 4.9 - 2
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 173634 None 0 Mouse Binding pIC50 = 4.9 4.9 - 2
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 15618 None 4 Human Binding pIC50 = 6.9 6.9 -12 8
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 15618 None 4 Human Binding pIC50 = 6.9 6.9 -12 8
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 15144 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 15144 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 146012 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 146012 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 217878 None 0 Human Binding pIC50 = 5.9 5.9 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3577981 214209 None 1 Mouse Binding pIC50 = 4.9 4.9 -29 2
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 None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL188738 211518 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL5087814 217609 None 0 Human Binding pIC50 = 6.9 6.9 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44448660 95026 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 95026 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 122496 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 122496 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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
44577515 189115 None 0 Human Binding pIC50 = 6.9 6.9 - 1
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 189115 None 0 Human Binding pIC50 = 6.9 6.9 - 1
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 15045 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 15045 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 60837 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60837 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 214704 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44277696 101259 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 101259 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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
6918813 131439 None 2 Human Binding pIC50 = 4.9 4.9 - 0
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 131439 None 2 Human Binding pIC50 = 4.9 4.9 - 0
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 101259 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 101259 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 118867 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 118867 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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
1324 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
16154396 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
16197727 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
16197727.0 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
44285019 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
57514683 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
91898441 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
DB04931 302 None 19 Mouse Binding pIC50 = 6.9 6.9 - 4
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 None None None None 10.1021/acs.jmedchem.9b00860
54584301 60830 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60830 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60831 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60831 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60832 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 60832 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 126295 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 126295 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 213938 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
15953838 67291 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 67291 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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
CHEMBL539306 67291 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 122493 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 122493 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 140756 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 140756 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 149141 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 149141 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 212620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
57854102 148409 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 148409 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 157914 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 157914 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
122184909 122620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 122620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 217205 None 0 Human Binding pIC50 = 5.8 5.8 - 3
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 None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168282779 191280 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 191280 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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
1338 3807 None 36 Rat Binding pIC50 = 5.8 5.8 - 4
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 3807 None 36 Rat Binding pIC50 = 5.8 5.8 - 4
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 3807 None 36 Rat Binding pIC50 = 5.8 5.8 - 4
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 211523 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL365794 214501 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL3600920 214283 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44347840 162018 None 0 Human Binding pIC50 = 7.8 7.8 -208 3
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 162018 None 0 Human Binding pIC50 = 7.8 7.8 -208 3
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 162018 None 0 Human Binding pIC50 = 7.8 7.8 -208 3
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 210963 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
CHEMBL3600840 214277 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600832 214273 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145973975 164752 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 164752 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 168982 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 168982 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 213864 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5090670 217767 None 0 Human Binding pIC50 = 6.8 6.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137636965 156307 None 0 Human Binding pIC50 = 4.8 4.8 - 3
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 156307 None 0 Human Binding pIC50 = 4.8 4.8 - 3
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 164442 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 164442 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 217613 None 0 Human Binding pIC50 = 6.8 6.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
118735100 118864 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 118864 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 214282 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5090946 217775 None 0 Human Binding pIC50 = 6.8 6.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445085 97127 None 0 Human Binding pIC50 = 7.8 7.8 2 2
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 97127 None 0 Human Binding pIC50 = 7.8 7.8 2 2
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 75427 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 75427 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 75534 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 75534 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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
132938008 159607 None 0 Mouse Binding pIC50 = 5.8 5.8 -17 2
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@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4102048 159607 None 0 Mouse Binding pIC50 = 5.8 5.8 -17 2
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@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
138106885 167007 None 49 Human Binding pIC50 = 4.8 4.8 -3 4
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 167007 None 49 Human Binding pIC50 = 4.8 4.8 -3 4
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 167007 None 49 Human Binding pIC50 = 4.8 4.8 -3 4
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 192455 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 192455 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 216882 None 0 Human Binding pIC50 = 6.8 6.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5077095 216967 None 0 Human Binding pIC50 = 6.8 6.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3601431 214287 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077144 216973 None 0 Human Binding pIC50 = 5.8 5.8 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16133793 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
44273719 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
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 None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16132144 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
16133793 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44273719 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.8 7.8 -100 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44408190 96976 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 96976 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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
71449047 78511 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 78511 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 188843 None 0 Human Binding pIC50 = 6.7 6.7 - 3
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 188843 None 0 Human Binding pIC50 = 6.7 6.7 - 3
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 141449 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 141449 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 213864 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
42630327 155961 None 0 Human Binding pIC50 = 5.7 5.7 - 3
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 155961 None 0 Human Binding pIC50 = 5.7 5.7 - 3
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 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 20 Human Binding pIC50 = 5.7 5.7 -19 5
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 None None None None 10.1021/acs.jmedchem.1c00095
10408 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
10408 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 23 Human Binding pIC50 = 6.7 6.7 -3 4
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 None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL5083551 217358 None 0 Human Binding pIC50 = 6.7 6.7 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5091236 217789 None 0 Human Binding pIC50 = 5.7 5.7 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190427 211524 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL190732 211526 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL191063 211538 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2371835 212596 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
168273822 190679 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 190679 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 212568 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2371971 212627 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O 10.1021/jm0614275
CHEMBL502300 216640 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
1324 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
16154396 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
16197727 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
16197727.0 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
44285019 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
57514683 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
91898441 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
DB04931 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
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 None None None None 10.1021/jm049579s
1324 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 19 Human Binding pIC50 = 8.7 8.7 -6 4
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL413573 215535 None 0 Human Binding pIC50 = 8.7 8.7 1 2
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
CHEMBL204263 211622 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL425591 215799 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
CHEMBL503229 216651 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL443071 216381 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL500743 216612 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2371967 212623 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
122184637 122502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 122502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 212619 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
145973779 164827 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 164827 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 140640 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 140640 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 216309 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44347927 157368 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 157368 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 14513 None 0 Human Binding pIC50 = 5.7 5.7 -1 4
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 216916 None 0 Human Binding pIC50 = 6.7 6.7 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44448590 95652 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 95652 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 97293 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 97293 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 212731 None 0 Human Binding pIC50 = 7.7 7.7 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
145967155 164338 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 164338 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 140410 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 140410 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 94907 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 94907 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 218036 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44408275 75446 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 75446 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 215207 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm0510326
1334 1501 None 4 Human Binding pIC50 = 5.7 5.7 -3 3
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 None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Binding pIC50 = 5.7 5.7 -3 3
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 None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Binding pIC50 = 5.7 5.7 -3 3
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 None None None None 10.1021/jm049579s
CHEMBL3600841 214278 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
4189 209380 None 58 Human Binding pIC50 = 4.7 4.7 -61 34
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
CHEMBL1559 209380 None 58 Human Binding pIC50 = 4.7 4.7 -61 34
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 209380 None 58 Human Binding pIC50 = 4.7 4.7 -61 34
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 505 None 55 Human Binding pIC50 = 5.6 5.6 -63 41
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
249 505 None 55 Human Binding pIC50 = 5.6 5.6 -63 41
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 505 None 55 Human Binding pIC50 = 5.6 5.6 -63 41
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 505 None 55 Human Binding pIC50 = 5.6 5.6 -63 41
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 505 None 55 Human Binding pIC50 = 5.6 5.6 -63 41
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
1323 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00170
24774438 94908 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 94908 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 123030 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 123030 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 212629 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL2115441 211727 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
6918813 131439 None 2 Human Binding pIC50 = 5.6 5.6 - 0
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 131439 None 2 Human Binding pIC50 = 5.6 5.6 - 0
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 95042 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 95042 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 15037 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 15037 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 214893 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
1334 1501 None 4 Human Binding pIC50 = 5.6 5.6 -3 3
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 4 Human Binding pIC50 = 5.6 5.6 -3 3
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 4 Human Binding pIC50 = 5.6 5.6 -3 3
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
137659790 159416 None 0 Human Binding pIC50 = 4.6 4.6 - 3
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 159416 None 0 Human Binding pIC50 = 4.6 4.6 - 3
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 122625 None 0 Human Binding pIC50 = 6.6 6.6 - 1
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 122625 None 0 Human Binding pIC50 = 6.6 6.6 - 1
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
1323 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 38 Human Binding pIC50 = 7.6 7.6 -346 4
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 None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL228194 211912 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
71456219 78778 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 78778 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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
5384 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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 3747 None 45 Human Binding pIC50 = 4.6 4.6 -66 35
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
CHEMBL2221249 211902 None 0 Human Binding pIC50 = 6.6 6.6 -1 3
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O nan
122184635 122500 None 0 Human Binding pIC50 = 6.6 6.6 -3 4
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 122500 None 0 Human Binding pIC50 = 6.6 6.6 -3 4
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 217790 None 0 Human Binding pIC50 = 5.6 5.6 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445083 154394 None 0 Human Binding pIC50 = 7.6 7.6 - 1
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 154394 None 0 Human Binding pIC50 = 7.6 7.6 - 1
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 214275 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
155544852 175043 None 0 Mouse Binding pIC50 = 5.6 5.6 -19 3
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 175043 None 0 Mouse Binding pIC50 = 5.6 5.6 -19 3
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 215810 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44348200 160290 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 160290 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 95123 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 95123 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 15066 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 15066 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 156617 None 0 Human Binding pIC50 = 6.6 6.6 - 3
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 156617 None 0 Human Binding pIC50 = 6.6 6.6 - 3
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 206519 None 50 Human Binding pIC50 = 4.5 4.5 -15 12
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(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 206519 None 50 Human Binding pIC50 = 4.5 4.5 -15 12
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(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
44431511 88100 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 88100 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 173913 None 0 Mouse Binding pIC50 = 4.5 4.5 -50 3
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 173913 None 0 Mouse Binding pIC50 = 4.5 4.5 -50 3
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 215616 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3600833 214274 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413439 215530 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL204864 211625 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
168278924 191175 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 191175 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 144273 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 144273 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 214676 None 1 Human Binding pIC50 = 6.5 6.5 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1775066 211340 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 None None None C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
CHEMBL382369 214765 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
CHEMBL5075506 216867 None 0 Human Binding pIC50 = 5.5 5.5 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
10282847 123031 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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 123031 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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 144273 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 144273 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 79012 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 79012 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 211520 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL275999 213285 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL370321 214627 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
1338 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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 3807 None 36 Human Binding pIC50 = 6.5 6.5 -154 4
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
1334 1501 None 4 Human Binding pIC50 = 6.5 6.5 -3 3
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 None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Binding pIC50 = 6.5 6.5 -3 3
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 None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Binding pIC50 = 6.5 6.5 -3 3
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 None None None None 10.1021/jm049579s
10210964 67264 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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 67264 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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
16157270 215013 None 15 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 215013 None 15 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44577520 188932 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 188932 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 214712 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(O)cc2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
16157270 215013 None 15 Human Binding pIC50 = 6.5 6.5 - 0
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 215013 None 15 Human Binding pIC50 = 6.5 6.5 - 0
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 None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL3600843 214280 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
57853943 146612 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 146612 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 211910 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155561116 175077 None 0 Mouse Binding pIC50 = 4.4 4.4 -10 3
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 175077 None 0 Mouse Binding pIC50 = 4.4 4.4 -10 3
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 166951 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 166951 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 118866 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 118866 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 102943 None 17 Human Binding pIC50 = 5.4 5.4 -478 16
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 102943 None 17 Human Binding pIC50 = 5.4 5.4 -478 16
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
CHEMBL334255 102943 None 17 Human Binding pIC50 = 5.4 5.4 -478 16
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 189218 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 189218 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 164728 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 164728 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 66225 None 0 Human Binding pIC50 = 6.4 6.4 61 4
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 66225 None 0 Human Binding pIC50 = 6.4 6.4 61 4
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 66707 None 0 Human Binding pIC50 = 6.4 6.4 27 3
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 66707 None 0 Human Binding pIC50 = 6.4 6.4 27 3
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 217969 None 0 Human Binding pIC50 = 6.4 6.4 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
122184638 122503 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 122503 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155741 None 2 Human Binding pIC50 = 5.4 5.4 - 1
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 155741 None 2 Human Binding pIC50 = 5.4 5.4 - 1
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 122501 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 122501 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 214692 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
8447 189057 None 54 Human Binding pIC50 = 5.4 5.4 -50 13
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 189057 None 54 Human Binding pIC50 = 5.4 5.4 -50 13
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 207971 None 50 Human Binding pIC50 = 4.4 4.4 -81 34
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
CHEMBL1201049 207971 None 50 Human Binding pIC50 = 4.4 4.4 -81 34
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 207971 None 50 Human Binding pIC50 = 4.4 4.4 -81 34
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 214630 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
1323 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.ejmech.2018.04.021
172445559 195459 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 195459 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 210965 None 0 Human Binding pIC50 = 8.4 8.4 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
44422999 168958 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 168958 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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
1323 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1021/ml500436s
92432 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1021/ml500436s
1323 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.4 8.4 -346 4
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 None None None None 10.1016/j.bmcl.2011.03.019
163196518 192238 None 3 Human Binding pIC50 = 8.4 8.4 - 0
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 192238 None 3 Human Binding pIC50 = 8.4 8.4 - 0
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 210964 None 0 Human Binding pIC50 = 8.3 8.3 - 2
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
44397455 123910 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 123910 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 195064 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 195064 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 214752 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
57854192 153138 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
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 153138 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
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
137655905 158920 None 0 Human Binding pIC50 = 5.4 5.4 - 3
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 158920 None 0 Human Binding pIC50 = 5.4 5.4 - 3
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 157189 None 0 Human Binding pIC50 = 5.4 5.4 - 3
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 157189 None 0 Human Binding pIC50 = 5.4 5.4 - 3
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 190632 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 190632 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 122622 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 122622 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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
1323 2688 None 38 Human Binding pIC50 = 7.4 7.4 -346 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 38 Human Binding pIC50 = 7.4 7.4 -346 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 38 Human Binding pIC50 = 7.4 7.4 -346 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None None 10.1021/jm960845e
9808801 60829 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 60829 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 214772 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
145966490 164457 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 164457 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155338 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155338 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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
68617 207985 None 33 Human Binding pIC50 = 5.3 5.3 -21 25
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
CHEMBL1709 207985 None 33 Human Binding pIC50 = 5.3 5.3 -21 25
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 207985 None 33 Human Binding pIC50 = 5.3 5.3 -21 25
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 166591 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 166591 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 190214 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 190214 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 66187 None 0 Human Binding pIC50 = 6.3 6.3 22 4
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 66187 None 0 Human Binding pIC50 = 6.3 6.3 22 4
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 214276 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL438920 216270 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2371970 212626 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C2CCCCC2)NC1=O 10.1021/jm0614275
CHEMBL438294 216227 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL203602 211619 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
44206252 149420 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 149420 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 211521 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL2371828 212592 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
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 None None None 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 190641 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 190641 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 217194 None 0 Human Binding pIC50 = 6.3 6.3 - 3
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 None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
44445084 160833 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 160833 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 66901 None 0 Human Binding pIC50 = 6.3 6.3 57 4
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 66901 None 0 Human Binding pIC50 = 6.3 6.3 57 4
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 127532 None 0 Human Binding pIC50 = 6.3 6.3 245 3
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 127532 None 0 Human Binding pIC50 = 6.3 6.3 245 3
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 79010 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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 79010 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human 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 60838 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 60838 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 121358 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 121358 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 215302 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5080489 217177 None 0 Human Binding pIC50 = 6.3 6.3 - 3
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 None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263948 213058 None 1 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960840h
16132144 211738 None 29 Human Binding pIC50 = 6.3 6.3 -100 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
16133793 211738 None 29 Human Binding pIC50 = 6.3 6.3 -100 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
44273719 211738 None 29 Human Binding pIC50 = 6.3 6.3 -100 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
CHEMBL214332 211738 None 29 Human Binding pIC50 = 6.3 6.3 -100 4
Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
57854192 153138 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 153138 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 172712 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 172712 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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
57854192 153138 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 153138 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 213864 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL3600922 214285 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24858629 197925 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 197925 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 159541 None 0 Human Binding pIC50 = 7.2 7.2 - 3
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 159541 None 0 Human Binding pIC50 = 7.2 7.2 - 3
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
145948876 167581 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 167581 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 217068 None 0 Human Binding pIC50 = 6.2 6.2 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL455070 216468 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
122184634 122499 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 122499 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 122494 None 0 Human Binding pIC50 = 8.2 8.2 - 1
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 122494 None 0 Human Binding pIC50 = 8.2 8.2 - 1
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 122459 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 122459 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 214281 None 0 Human Binding pIC50 = 8.2 8.2 - 1
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184633 122498 None 0 Human Binding pIC50 = 8.2 8.2 - 1
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 122498 None 0 Human Binding pIC50 = 8.2 8.2 - 1
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 214272 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
49862377 15047 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 15047 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 163853 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 163853 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 140431 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 140431 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 66915 None 0 Human Binding pIC50 = 6.2 6.2 38 3
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 66915 None 0 Human Binding pIC50 = 6.2 6.2 38 3
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 217971 None 0 Human Binding pIC50 = 6.2 6.2 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190953 211536 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL364711 214492 None 0 Mouse Binding pIC50 = 5.2 5.2 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
118735099 118863 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 118863 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 215339 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
10304547 168355 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 168355 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 9782 None 0 Human Binding pIC50 = 5.2 5.2 -2 4
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 126849 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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
CHEMBL365401 126849 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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
44448629 167561 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 167561 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 211957 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
10257242 15036 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 15036 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 156191 None 0 Human Binding pIC50 = 5.2 5.2 - 3
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 156191 None 0 Human Binding pIC50 = 5.2 5.2 - 3
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 155461 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 155461 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 217743 None 0 Human Binding pIC50 = 6.2 6.2 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263822 213049 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
168295131 192351 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 192351 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 79007 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 79007 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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
1323 2688 None 38 Human Binding pIC50 = 8.2 8.2 -346 4
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 None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 38 Human Binding pIC50 = 8.2 8.2 -346 4
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 None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.2 8.2 -346 4
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 None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL2371969 212625 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0614275
CHEMBL393075 214922 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm070461w
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm070461w
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.5b01285
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm060768f
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm060768f
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm801300c
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
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 None None None None 10.1021/jm801300c
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -346 4
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
11375764 66710 None 0 Human Binding pIC50 = 7.2 7.2 398 3
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 66710 None 0 Human Binding pIC50 = 7.2 7.2 398 3
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 214731 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
118735101 118865 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 118865 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 212628 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](CC2CCC(C3CCCCC3)CC2)NC(=O)[C@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
137641157 157156 None 0 Human Binding pIC50 = 6.2 6.2 - 1
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 157156 None 0 Human Binding pIC50 = 6.2 6.2 - 1
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 158699 None 0 Human Binding pIC50 = 5.2 5.2 - 3
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 158699 None 0 Human Binding pIC50 = 5.2 5.2 - 3
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 211685 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5093939 217948 None 0 Human Binding pIC50 = 6.1 6.1 - 1
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
71456220 78779 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 78779 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 159311 None 0 Human Binding pIC50 = 6.1 6.1 - 3
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 159311 None 0 Human Binding pIC50 = 6.1 6.1 - 3
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 172558 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 172558 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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
2726.0 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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
621 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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
83 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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 919 None 48 Human Binding pIC50 = 5.1 5.1 -112 72
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 213864 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
168295644 192421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 192421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 211911 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
24774358 154994 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 154994 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 211516 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
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 None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL191120 211539 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
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 None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
122184910 122621 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 122621 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 140755 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 140755 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 124424 None 0 Human Binding pIC50 = 7.1 7.1 53 3
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 124424 None 0 Human Binding pIC50 = 7.1 7.1 53 3
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 158408 None 0 Human Binding pIC50 = 6.1 6.1 - 1
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 158408 None 0 Human Binding pIC50 = 6.1 6.1 - 1
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 8395 None 6 Human Binding pIC50 = 7.1 7.1 - 0
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 8395 None 6 Human Binding pIC50 = 7.1 7.1 - 0
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 124426 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 124426 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60828 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60828 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 213864 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
137658158 159811 None 0 Human Binding pIC50 = 5.1 5.1 - 3
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 159811 None 0 Human Binding pIC50 = 5.1 5.1 - 3
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 145897 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 145897 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 154391 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 154391 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 214284 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5087839 217610 None 0 Human Binding pIC50 = 7.1 7.1 - 3
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 None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
127053936 152329 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 152329 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 214279 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
168285801 191590 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 191590 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96696 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96696 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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
71452720 79002 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 79002 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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
1337 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
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 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
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 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
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
176 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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
2157.0 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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 398 None 47 Human Binding pIC50 = 5.0 5.0 -5 31
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 122495 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 122495 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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
3372.0 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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 1662 None 37 Human Binding pIC50 = 5.0 5.0 -416 65
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 97218 None 0 Human Binding pIC50 = 4.0 4.0 - 0
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 97218 None 0 Human Binding pIC50 = 4.0 4.0 - 0
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 67453 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 67453 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 216377 None 0 Human Binding pKi = 10.1 10.1 -1 3
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 None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL415165 215636 None 0 Human Binding pKi = 9.8 9.8 -1 5
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 None None None None 10.1021/jm0501432
CHEMBL414718 215611 None 0 Human Binding pKi = 9.6 9.6 -2 4
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 None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
CHEMBL408843 215195 None 0 Human Binding pKi = 9.4 9.4 1 3
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 None None None CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
57646411 76949 None 0 Human Binding pKi = 9.3 9.3 -1 4
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 76949 None 0 Human Binding pKi = 9.3 9.3 -1 4
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
1324 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
16154396 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
16197727 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
16197727.0 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
44285019 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
57514683 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
91898441 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
CHEMBL441738 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
DB04931 302 None 19 Human Binding pKi = 9.3 9.3 -6 4
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 None None None None 10.1021/jm201489a
CHEMBL1923667 211547 None 0 Human Binding pKi = 9.2 9.2 1 3
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](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 211546 None 0 Human Binding pKi = 9.1 9.1 -1 3
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 None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](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 213165 None 0 Human Binding pKi = 9.1 9.1 -3 4
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 None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0501432
CHEMBL2370964 212426 None 0 Human Binding pKi = 9 9.0 -1 3
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
57646437 76950 None 0 Human Binding pKi = 8.9 8.9 -10 4
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 76950 None 0 Human Binding pKi = 8.9 8.9 -10 4
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 76950 None 0 Human Binding pKi = 8.9 8.9 -10 4
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 76950 None 0 Human Binding pKi = 8.9 8.9 -10 4
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 69095 None 0 Human Binding pKi = 8.9 8.9 1 3
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 69095 None 0 Human Binding pKi = 8.9 8.9 1 3
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 69095 None 0 Human Binding pKi = 8.9 8.9 1 3
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 69095 None 0 Human Binding pKi = 8.9 8.9 1 3
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 76948 None 0 Human Binding pKi = 8.8 8.8 -13 4
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 76948 None 0 Human Binding pKi = 8.8 8.8 -13 4
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 76953 None 0 Human Binding pKi = 8 8.0 -58 4
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 76953 None 0 Human Binding pKi = 8 8.0 -58 4
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 76953 None 0 Human Binding pKi = 8 8.0 -58 4
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 76953 None 0 Human Binding pKi = 8 8.0 -58 4
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 195544 None 0 Mouse Binding pKi = 6 6.0 -158 3
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 195544 None 0 Mouse Binding pKi = 6 6.0 -158 3
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 66845 None 0 Human Binding pKi = 6 6.0 -48 4
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 66845 None 0 Human Binding pKi = 6 6.0 -48 4
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 66891 None 0 Human Binding pKi = 6 6.0 -70 4
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 66891 None 0 Human Binding pKi = 6 6.0 -70 4
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 80120 None 0 Human Binding pKi = 6 6.0 -39 4
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 80120 None 0 Human Binding pKi = 6 6.0 -39 4
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 80120 None 0 Human Binding pKi = 6 6.0 -39 4
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 80120 None 0 Human Binding pKi = 6 6.0 -39 4
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 66845 None 0 Human Binding pKi = 6 6.0 -48 4
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 66845 None 0 Human Binding pKi = 6 6.0 -48 4
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 177177 None 0 Human Binding pKi = 5 5.0 -5 4
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 177177 None 0 Human Binding pKi = 5 5.0 -5 4
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 89631 None 0 Human Binding pKi = 5 5.0 -7 3
Displacement of [125I]NDP-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 89631 None 0 Human Binding pKi = 5 5.0 -7 3
Displacement of [125I]NDP-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 90076 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-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 90076 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-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 146397 None 0 Human Binding pKi = 5 5.0 -1 4
Displacement of [125I]NDP-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 146397 None 0 Human Binding pKi = 5 5.0 -1 4
Displacement of [125I]NDP-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 146556 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-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 146556 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-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 148236 None 0 Human Binding pKi = 5 5.0 -4 4
Displacement of [125I]NDP-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 148236 None 0 Human Binding pKi = 5 5.0 -4 4
Displacement of [125I]NDP-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 79181 None 0 Human Binding pKi = 5 5.0 -6 4
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 79181 None 0 Human Binding pKi = 5 5.0 -6 4
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 208029 None 2 Human Binding pKi = 4 4.0 - 1
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 208029 None 2 Human Binding pKi = 4 4.0 - 1
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 67207 None 0 Human Binding pKi = 6.0 6.0 - 1
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 67207 None 0 Human Binding pKi = 6.0 6.0 - 1
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 124424 None 0 Human Binding pKi = 8.0 8.0 53 3
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 124424 None 0 Human Binding pKi = 8.0 8.0 53 3
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 211645 None 0 Human Binding pKi = 7.0 7.0 -14 4
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 None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577062 193483 None 0 Human Binding pKi = 7.0 7.0 -26 3
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 193483 None 0 Human Binding pKi = 7.0 7.0 -26 3
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 178771 None 0 Human Binding pKi = 6.0 6.0 -109 3
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 178771 None 0 Human Binding pKi = 6.0 6.0 -109 3
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 188158 None 0 Human Binding pKi = 6.0 6.0 -316 7
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 188158 None 0 Human Binding pKi = 6.0 6.0 -316 7
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 88559 None 0 Human Binding pKi = 5.0 5.0 -5 4
Displacement of [125I]NDP-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 88559 None 0 Human Binding pKi = 5.0 5.0 -5 4
Displacement of [125I]NDP-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 88735 None 0 Human Binding pKi = 5.0 5.0 -3 3
Displacement of [125I]NDP-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 88735 None 0 Human Binding pKi = 5.0 5.0 -3 3
Displacement of [125I]NDP-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 89770 None 0 Human Binding pKi = 5.0 5.0 -4 4
Displacement of [125I]NDP-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 89770 None 0 Human Binding pKi = 5.0 5.0 -4 4
Displacement of [125I]NDP-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 90270 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-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 90270 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-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 90282 None 0 Human Binding pKi = 5.0 5.0 -6 4
Displacement of [125I]NDP-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 90282 None 0 Human Binding pKi = 5.0 5.0 -6 4
Displacement of [125I]NDP-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 148690 None 0 Human Binding pKi = 5.0 5.0 1 4
Displacement of [125I]NDP-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 148690 None 0 Human Binding pKi = 5.0 5.0 1 4
Displacement of [125I]NDP-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 151432 None 0 Human Binding pKi = 5.0 5.0 -17 4
Displacement of [125I]NDP-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 151432 None 0 Human Binding pKi = 5.0 5.0 -17 4
Displacement of [125I]NDP-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 15618 None 4 Human Binding pKi = 6.9 6.9 -12 8
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 15618 None 4 Human Binding pKi = 6.9 6.9 -12 8
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 191015 None 0 Human Binding pKi = 6.9 6.9 -1 4
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 191015 None 0 Human Binding pKi = 6.9 6.9 -1 4
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 212428 None 0 Human Binding pKi = 6.9 6.9 28 3
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
9960253 117013 None 0 Human Binding pKi = 5.9 5.9 -5 4
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 117013 None 0 Human Binding pKi = 5.9 5.9 -5 4
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 118011 None 0 Human Binding pKi = 5.9 5.9 -50 3
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 118011 None 0 Human Binding pKi = 5.9 5.9 -50 3
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 80177 None 0 Human Binding pKi = 5.9 5.9 -10 3
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 80177 None 0 Human Binding pKi = 5.9 5.9 -10 3
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 166596 None 0 Human Binding pKi = 5.9 5.9 -223 5
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 166596 None 0 Human Binding pKi = 5.9 5.9 -223 5
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 140468 None 0 Human Binding pKi = 5.9 5.9 -165 4
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 140468 None 0 Human Binding pKi = 5.9 5.9 -165 4
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 148282 None 0 Human Binding pKi = 5.9 5.9 -478 4
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 148282 None 0 Human Binding pKi = 5.9 5.9 -478 4
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 126612 None 0 Human Binding pKi = 5.9 5.9 -109 3
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 126612 None 0 Human Binding pKi = 5.9 5.9 -109 3
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 88635 None 0 Human Binding pKi = 4.9 4.9 -5 4
Displacement of [125I]NDP-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 88635 None 0 Human Binding pKi = 4.9 4.9 -5 4
Displacement of [125I]NDP-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 88648 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [125I]NDP-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 88648 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [125I]NDP-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 89286 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-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 89286 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-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 89535 None 0 Human Binding pKi = 4.9 4.9 -9 4
Displacement of [125I]NDP-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 89535 None 0 Human Binding pKi = 4.9 4.9 -9 4
Displacement of [125I]NDP-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 89548 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89548 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89953 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89953 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 167147 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-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 167147 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-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 79147 None 0 Human Binding pKi = 4.9 4.9 -1 4
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 79147 None 0 Human Binding pKi = 4.9 4.9 -1 4
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 211646 None 0 Human Binding pKi = 7.9 7.9 -22 4
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 None None None CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577092 178750 None 0 Human Binding pKi = 7.9 7.9 -11 3
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 178750 None 0 Human Binding pKi = 7.9 7.9 -11 3
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 114487 None 0 Human Binding pKi = 6.9 6.9 -346 3
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 114487 None 0 Human Binding pKi = 6.9 6.9 -346 3
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 153132 None 0 Human Binding pKi = 5.9 5.9 -676 3
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 153132 None 0 Human Binding pKi = 5.9 5.9 -676 3
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
164620129 185853 None 0 Mouse Binding pKi = 5.9 5.9 -64 3
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 185853 None 0 Mouse Binding pKi = 5.9 5.9 -64 3
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 196162 None 0 Mouse Binding pKi = 5.9 5.9 -81 3
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 196162 None 0 Mouse Binding pKi = 5.9 5.9 -81 3
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 88686 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [125I]NDP-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 88686 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [125I]NDP-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 88729 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 88729 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89813 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89813 None 0 Human Binding pKi = 4.9 4.9 1 3
Displacement of [125I]NDP-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 89850 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-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 89850 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-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 191895 None 0 Human Binding pKi = 6.9 6.9 -10 4
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 191895 None 0 Human Binding pKi = 6.9 6.9 -10 4
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 212430 None 0 Human Binding pKi = 7.9 7.9 -70 3
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44347331 16334 None 0 Human Binding pKi = 6.9 6.9 -257 3
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 16334 None 0 Human Binding pKi = 6.9 6.9 -257 3
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 168159 None 0 Human Binding pKi = 6.9 6.9 -11 3
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 168159 None 0 Human Binding pKi = 6.9 6.9 -11 3
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 120038 None 0 Human Binding pKi = 5.9 5.9 -23 3
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 120038 None