Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
1324 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16154396 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16197727 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
44285019 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
57514683 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
91898441 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
CHEMBL441738 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
DB04931 299 23 None -5 9 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
CHEMBL2371966 208408 0 None 616 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 115725 0 None 1 4 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358545 115725 0 None 1 4 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722941 115729 0 None 1 4 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358549 115729 0 None 1 4 Mouse 10.4 pEC50 = 10.4 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722933 115722 0 None 1 4 Mouse 10.3 pEC50 = 10.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358541 115722 0 None 1 4 Mouse 10.3 pEC50 = 10.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16154396 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16197727 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
44285019 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
57514683 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
91898441 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL441738 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
DB04931 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
1324 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
16154396 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
16197727 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
44285019 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
57514683 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
91898441 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
CHEMBL441738 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
DB04931 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL None None None None 10.1021/jm030452x
118722944 115732 0 None -1 4 Mouse 10.2 pEC50 = 10.2 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358552 115732 0 None -1 4 Mouse 10.2 pEC50 = 10.2 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
16154396 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
16197727 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
44285019 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
57514683 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
91898441 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL441738 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
DB04931 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL None None None None 10.1021/jm010524p
1324 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 299 23 None -5 9 Mouse 10.2 pEC50 = 10.2 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL414965 211408 0 None -1 5 Mouse 10.1 pEC50 = 10.1 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16154396 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
44285019 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
57514683 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
91898441 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
CHEMBL441738 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
DB04931 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
1324 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
16154396 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
44285019 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
57514683 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
91898441 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
CHEMBL441738 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
DB04931 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm0490843
1324 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16154396 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16197727 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
44285019 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
57514683 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
91898441 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
CHEMBL441738 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
DB04931 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
118722930 115720 0 None 1 4 Mouse 10.1 pEC50 = 10.1 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358539 115720 0 None 1 4 Mouse 10.1 pEC50 = 10.1 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 299 23 None -5 9 Mouse 10.1 pEC50 = 10.1 Functional
Functional activity at the mouse melanocortin 5 receptorFunctional activity at the mouse melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL405087 210784 0 None -1 5 Mouse 10.0 pEC50 = 10 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16154396 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
44285019 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
57514683 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
91898441 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
CHEMBL441738 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
DB04931 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
1324 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16154396 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16197727 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
44285019 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
57514683 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
91898441 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL441738 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
DB04931 299 23 None -5 9 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL406842 210867 0 None 3 5 Mouse 10.0 pEC50 = 10.0 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 211297 0 None -6 4 Mouse 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 135909 0 None -2 4 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 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 135909 0 None -2 4 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 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 211062 0 None 11 5 Mouse 9.9 pEC50 = 9.9 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 115717 0 None -1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358535 115717 0 None -1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
118722931 115721 0 None 1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358540 115721 0 None 1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
118722938 115726 0 None -1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358546 115726 0 None -1 4 Mouse 9.9 pEC50 = 9.9 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16154396 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
44285019 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
57514683 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
91898441 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
DB04931 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
127036484 135909 0 None -2 4 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 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 135909 0 None -2 4 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 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 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
16154396 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
16197727 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
44285019 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
57514683 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
91898441 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
CHEMBL441738 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
DB04931 299 23 None -5 9 Mouse 9.9 pEC50 = 9.9 Functional
Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayInverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00684
CHEMBL411400 211126 0 None 48 5 Mouse 9.9 pEC50 = 9.9 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 115730 0 None -1 4 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358550 115730 0 None -1 4 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722943 115731 0 None -1 4 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358551 115731 0 None -1 4 Mouse 9.8 pEC50 = 9.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1323 2639 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2639 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2639 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 81162 0 None -7 4 Mouse 9.8 pEC50 = 9.8 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
CHEMBL216295 81162 0 None -7 4 Mouse 9.8 pEC50 = 9.8 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
CHEMBL2371851 208384 0 None -3 4 Mouse 9.8 pEC50 = 9.8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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
1324 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16154396 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
44285019 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
57514683 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
91898441 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL441738 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
DB04931 299 23 None -5 9 Mouse 9.8 pEC50 = 9.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL405335 210799 0 None 2 4 Mouse 9.8 pEC50 = 9.8 Functional
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 115718 0 None 1 4 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358536 115718 0 None 1 4 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
122194229 123452 0 None -7 5 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 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 123452 0 None -7 5 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 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 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16154396 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
44285019 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
57514683 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
91898441 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL441738 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
DB04931 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
1323 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
92432 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL430239 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
1324 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16154396 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16197727 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
44285019 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
57514683 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
91898441 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
CHEMBL441738 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
DB04931 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
1323 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
92432 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
CHEMBL430239 2639 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16154396 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16197727 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
44285019 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
57514683 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
91898441 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
CHEMBL441738 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
DB04931 299 23 None -5 9 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16132144 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 210978 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 115006 0 None 1 4 Mouse 9.6 pEC50 = 9.6 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3352878 115006 0 None 1 4 Mouse 9.6 pEC50 = 9.6 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL2371969 208411 0 None 1000 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16154396 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
44285019 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
57514683 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
91898441 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
DB04931 299 23 None -14 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
1324 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
16154396 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
16197727 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
44285019 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
57514683 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
91898441 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
CHEMBL441738 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
DB04931 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
1324 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16154396 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16197727 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
44285019 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
57514683 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
91898441 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL441738 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
DB04931 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
122194229 123452 0 None -7 5 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 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 123452 0 None -7 5 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 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 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16154396 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16197727 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
44285019 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
57514683 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
91898441 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
CHEMBL441738 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
DB04931 299 23 None -5 9 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
CHEMBL2371971 208413 0 None 1288 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 212360 0 None 37 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 158693 0 None 3 4 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4099127 158693 0 None 3 4 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
1324 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16154396 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16197727 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
44285019 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
57514683 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
91898441 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
CHEMBL441738 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
DB04931 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
1324 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16154396 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
44285019 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
57514683 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
91898441 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL441738 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
DB04931 299 23 None -5 9 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
45487403 195749 0 None -33 5 Mouse 9.5 pEC50 = 9.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569693 195749 0 None -33 5 Mouse 9.5 pEC50 = 9.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
118722936 115724 0 None -3 4 Mouse 9.5 pEC50 = 9.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358544 115724 0 None -3 4 Mouse 9.5 pEC50 = 9.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL2371962 208404 0 None 8 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 208978 0 None -11 4 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 299 23 None -14 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16132144 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 299 23 None -5 9 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16132144 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 209225 0 None 10 4 Mouse 9.4 pEC50 = 9.4 Functional
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 208928 0 None -12 6 Mouse 9.4 pEC50 = 9.4 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207524 31 None -1 8 Mouse 9.4 pEC50 = 9.4 Functional
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 208409 0 None 275 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 156105 0 None -1 4 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4069451 156105 0 None -1 4 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
90643803 111238 0 None 1 5 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111238 0 None 1 5 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL386081 210618 0 None -25 4 Mouse 9.3 pEC50 = 9.3 Functional
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 211758 0 None -21 4 Mouse 9.3 pEC50 = 9.3 Functional
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 118639 0 None 1 5 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
CHEMBL342954 118639 0 None 1 5 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
16132144 207524 31 None -1 8 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 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 211081 0 None -14 4 Mouse 9.3 pEC50 = 9.3 Functional
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 207872 0 None -2 4 Mouse 9.3 pEC50 = 9.3 Functional
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 211124 0 None 16 5 Mouse 9.3 pEC50 = 9.3 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 96867 0 None -3 4 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
77231883 96867 0 None -3 4 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL269274 96867 0 None -3 4 Mouse 9.3 pEC50 = 9.3 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
10078903 67662 0 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191303 67662 0 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
1324 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
16154396 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
44285019 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
57514683 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
91898441 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
DB04931 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
1324 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
16154396 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
44285019 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
57514683 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
91898441 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
DB04931 299 23 None -14 9 Human 9.2 pEC50 = 9.2 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960840h
16132144 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 208872 2 None -13 4 Mouse 9.2 pEC50 = 9.2 Functional
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 111241 0 None 6 5 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111241 0 None 6 5 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL428801 211714 0 None -12 5 Mouse 9.2 pEC50 = 9.2 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
16131138 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
44349184 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
53310908 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
91898438 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL438402 168319 17 None -1 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
16132144 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.2 pEC50 = 9.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 122027 0 None 2 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122027 0 None 2 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
16132144 207524 31 None -1 8 Mouse 9.1 pEC50 = 9.1 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.1 pEC50 = 9.1 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.1 pEC50 = 9.1 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 207524 31 None -1 8 Mouse 9.1 pEC50 = 9.1 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 111237 0 None 2 5 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111237 0 None 2 5 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
11158573 70760 0 None -2 4 Mouse 9.1 pEC50 = 9.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL195439 70760 0 None -2 4 Mouse 9.1 pEC50 = 9.1 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
137637283 155427 0 None -2 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 155427 0 None -2 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC5R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL2371968 208410 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 208412 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 111242 0 None 7 5 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111242 0 None 7 5 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
1324 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1324 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16154396 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
44285019 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
57514683 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
91898441 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
DB04931 299 23 None -14 9 Human 9.0 pEC50 = 9 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
1324 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16154396 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
44285019 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
57514683 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
91898441 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL441738 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
DB04931 299 23 None -14 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
122184635 121906 0 None 2 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 121906 0 None 2 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
90643804 111239 0 None 2 5 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111239 0 None 2 5 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
16132144 207524 31 None -1 8 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 207524 31 None -1 8 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 207452 0 None 1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 211702 0 None -70 5 Mouse 8.9 pEC50 = 8.9 Functional
Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptorEvaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor
ChEMBL 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 173601 0 None -4 4 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4547556 173601 0 None -4 4 Mouse 8.9 pEC50 = 8.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL1688107 207081 0 None -8 4 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 212296 0 None -3 5 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
92432 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL2371963 208405 0 None 295 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 212343 0 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 209478 0 None 2 4 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 173755 0 None 6 4 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550976 173755 0 None 6 4 Mouse 8.8 pEC50 = 8.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
1323 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2639 49 None -181 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
118722939 115727 0 None -3 4 Mouse 8.8 pEC50 = 8.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358547 115727 0 None -3 4 Mouse 8.8 pEC50 = 8.8 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL2370966 208214 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 115728 0 None -2 4 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358548 115728 0 None -2 4 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358537 209812 0 None -7 4 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 163195 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 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 163195 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 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 212382 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 212162 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 115723 0 None -1 4 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358543 115723 0 None -1 4 Mouse 8.7 pEC50 = 8.7 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1324 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16154396 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16197727 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
44285019 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
57514683 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
91898441 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
CHEMBL441738 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
DB04931 299 23 None -5 9 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
11787684 69916 0 None -3 4 Mouse 8.0 pEC50 = 8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL194217 69916 0 None -3 4 Mouse 8.0 pEC50 = 8 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3752534 210459 1 None -25 4 Human 8.0 pEC50 = 8 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 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 60472 0 None -87 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 60472 0 None -87 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
49862377 14857 0 None -40 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 14857 0 None -40 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
137632948 156029 0 None -4 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4068643 156029 0 None -4 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
44401319 12161 0 None -19 2 Human 6.0 pEC50 = 6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1184826 12161 0 None -19 2 Human 6.0 pEC50 = 6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL2028959 12161 0 None -19 2 Human 6.0 pEC50 = 6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL407213 210891 0 None - 1 Human 6.0 pEC50 = 6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 173930 0 None -77 3 Mouse 5.0 pEC50 = 5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4555150 173930 0 None -77 3 Mouse 5.0 pEC50 = 5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
11017471 31686 0 None -295 2 Human 6.0 pEC50 = 6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1 10.1021/jm025539h
CHEMBL140738 31686 0 None -295 2 Human 6.0 pEC50 = 6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1 10.1021/jm025539h
44448629 166892 0 None -28 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 166892 0 None -28 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL50056 212338 2 None -8 7 Mouse 7.0 pEC50 = 7.0 Functional
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 212338 2 None -8 7 Mouse 7.0 pEC50 = 7.0 Functional
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 185269 0 None - 1 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 13 3 3 5.8 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4867949 185269 0 None - 1 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 13 3 3 5.8 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
45487296 195639 0 None -8 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568836 195639 0 None -8 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
45487416 195332 0 None -9 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567039 195332 0 None -9 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL3600833 210057 0 None -9 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 155928 0 None -38 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 155928 0 None -38 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL264190 208853 1 None 2 8 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 174713 0 None -2 4 Mouse 8.0 pEC50 = 8.0 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4573041 174713 0 None -2 4 Mouse 8.0 pEC50 = 8.0 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL319871 209468 0 None 2 4 Mouse 7.9 pEC50 = 7.9 Functional
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 207762 0 None 4 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 93602 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 506 7 2 4 4.3 CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248892 93602 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 506 7 2 4 4.3 CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44441685 93685 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249322 93685 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL319922 209469 0 None 1 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 208744 0 None -177 4 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 206703 0 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 195750 0 None -2344 5 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569694 195750 0 None -2344 5 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44408388 139780 0 None -45 4 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 139780 0 None -45 4 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
155547842 173114 0 None -50 4 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4535510 173114 0 None -50 4 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44448479 154820 0 None -9 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 154820 0 None -9 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
44310242 155756 0 None 16 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932912 155756 0 None 16 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL406550 155756 0 None 16 3 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL2323529 207755 0 None -1 4 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 190875 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 190875 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
164623712 185065 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 13 3 3 5.3 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4864765 185065 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 13 3 3 5.3 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
11061068 31062 0 None -295 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 31062 0 None -295 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
45487407 195283 0 None -7 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566545 195283 0 None -7 3 Mouse 4.9 pEC50 = 4.9 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
155561743 175189 0 None 3 4 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4583714 175189 0 None 3 4 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155566298 175210 0 None 3 4 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4584189 175210 0 None 3 4 Mouse 7.9 pEC50 = 7.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
164624151 185206 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866885 185206 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164626157 185800 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4875776 185800 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
137653704 158075 0 None -3 4 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4092424 158075 0 None -3 4 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155550338 173726 0 None -18 3 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173726 0 None -18 3 Mouse 5.9 pEC50 = 5.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 207838 0 None -3 4 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 156205 0 None -81 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 156205 0 None -81 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
145966490 163799 0 None -3 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 163799 0 None -3 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145975465 163386 0 None -23 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 163386 0 None -23 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
164623811 185308 0 None 1 4 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868636 185308 0 None 1 4 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
155538472 172670 0 None 2 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4524668 172670 0 None 2 3 Mouse 6.9 pEC50 = 6.9 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL427629 211599 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 60473 0 None -53 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 60473 0 None -53 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
44401315 12160 0 None -48 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1184825 12160 0 None -48 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL2028957 12160 0 None -48 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
90661465 76794 0 None -46 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2028958 76794 0 None -46 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2078649 76794 0 None -46 2 Human 5.9 pEC50 = 5.9 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2304247 207729 0 None -229 4 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 214013 0 None -2 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 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 7859 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
CHEMBL1090484 7859 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
44305885 201390 0 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 474 13 4 4 3.5 NCCCCNC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL63867 201390 0 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 474 13 4 4 3.5 NCCCCNC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
122184911 122028 0 None -8 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122028 0 None -8 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
16132144 207524 31 None -1 8 Mouse 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 207524 31 None -1 8 Mouse 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 207524 31 None -1 8 Mouse 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 207524 31 None -1 8 Mouse 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 183962 0 None 1 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 183962 0 None 1 3 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 207698 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 8372 0 None -41 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1093858 8372 0 None -41 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL3601431 210070 0 None 1 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 121899 0 None -2 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 121899 0 None -2 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
51350911 58481 0 None -2 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322399 58481 0 None -2 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932357 58481 0 None -2 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688109 58481 0 None -2 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL602651 214031 0 None -1 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 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 182311 0 None 3 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4792291 182311 0 None 3 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
137648053 156985 0 None 3 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4080169 156985 0 None 3 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL343094 209941 0 None 1 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 94535 0 None -186 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 94535 0 None -186 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
164613912 184168 0 None 6 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 12 3 3 4.9 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4851040 184168 0 None 6 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 12 3 3 4.9 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
137640475 156533 0 None -36 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4074368 156533 0 None -36 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
46232220 199359 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602652 199359 0 None -4 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487295 195688 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569221 195688 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44448590 95142 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95142 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL432895 211877 2 None 1 4 Mouse 5.8 pEC50 = 5.8 Functional
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 210069 0 None -17 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 210056 0 None -3 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 208407 0 None 331 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 155618 0 None -23 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4063911 155618 0 None -23 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
16132144 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 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 207524 31 None -81 8 Human 7.8 pEC50 = 7.8 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 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 212208 0 None -1 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 163478 0 None -10 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 163478 0 None -10 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1324 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16154396 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16197727 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
44285019 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
57514683 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
91898441 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
CHEMBL441738 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
DB04931 299 23 None -5 9 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
10146211 63983 0 None -61 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 63983 0 None -61 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
44347221 16442 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 16442 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
9852256 174785 0 None -4 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4574756 174785 0 None -4 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
164609931 183905 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 12 3 3 5.6 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4847357 183905 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 529 12 3 3 5.6 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
44457021 97439 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL272439 97439 0 None -9 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
44441646 153542 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 153542 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487288 195670 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569076 195670 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
46885815 7763 0 None -389 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
CHEMBL1089830 7763 0 None -389 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
145964837 163784 0 None -3 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 163784 0 None -3 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
137656489 159151 0 None 1 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4104402 159151 0 None 1 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
162666503 181638 0 None -16 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 181638 0 None -16 3 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 174454 0 None 5 4 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567480 174454 0 None 5 4 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
132180653 174477 0 None -17 3 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 174477 0 None -17 3 Mouse 7.8 pEC50 = 7.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 211484 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 211594 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 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 185287 0 None 2 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868223 185287 0 None 2 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
44431512 145379 0 None -5 4 Human 6.8 pEC50 = 6.8 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 145379 0 None -5 4 Human 6.8 pEC50 = 6.8 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
46885759 8177 0 None -295 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092548 8177 0 None -295 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
164628926 185921 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 14 3 3 6.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4877537 185921 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 14 3 3 6.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL3349030 209649 0 None -8 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 78543 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL2113028 78543 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
155538874 172211 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4513460 172211 0 None 1 3 Mouse 5.8 pEC50 = 5.8 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137649203 156954 0 None -10 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079721 156954 0 None -10 3 Mouse 4.8 pEC50 = 4.8 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
45487289 195675 0 None -10 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 590 17 8 7 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccnc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569104 195675 0 None -10 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 590 17 8 7 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccnc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2304250 207731 0 None -2 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 211866 0 None 1 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 195169 0 None -5 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL565927 195169 0 None -5 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
164616640 183972 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 13 3 3 6.0 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4848447 183972 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 543 13 3 3 6.0 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL268851 209014 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 78056 0 None -40 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 78056 0 None -40 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44401323 11680 0 None -72 2 Human 5.7 pEC50 = 5.7 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 569 7 4 5 3.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1181891 11680 0 None -72 2 Human 5.7 pEC50 = 5.7 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 569 7 4 5 3.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL2028961 11680 0 None -72 2 Human 5.7 pEC50 = 5.7 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 569 7 4 5 3.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
6918813 130836 2 None -398 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 130836 2 None -398 4 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
45487291 195687 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569220 195687 0 None -6 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
11328898 7863 18 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 7863 18 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1204059 7863 18 None -165 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44441687 93558 0 None -43 2 Human 5.7 pEC50 = 5.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.3 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL248671 93558 0 None -43 2 Human 5.7 pEC50 = 5.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.3 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1 10.1016/j.bmcl.2006.11.084
44396986 67078 0 None -43 3 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 67078 0 None -43 3 Human 5.7 pEC50 = 5.7 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2304246 207728 0 None -3 3 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 164070 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 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 164070 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 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 97502 0 None 1 5 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL272660 97502 0 None 1 5 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
16132144 207524 31 None -1 8 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 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 207524 31 None -1 8 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 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 207524 31 None -1 8 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 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 207524 31 None -1 8 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 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 212172 0 None -4 4 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 139095 0 None 2 5 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3797690 139095 0 None 2 5 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
137656180 158470 0 None 5 4 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4096678 158470 0 None 5 4 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
155543031 172600 0 None -3 4 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4522298 172600 0 None -3 4 Mouse 8.7 pEC50 = 8.7 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL406891 210869 0 None 2 5 Mouse 8.7 pEC50 = 8.7 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 207081 0 None -8 4 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 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 3530 12 None -3 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
6440621 3530 12 None -3 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
9898183 3530 12 None -3 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
CHEMBL3422426 3530 12 None -3 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
CHEMBL3287327 209554 0 None 1 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 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 125143 0 None -2 4 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL364726 125143 0 None -2 4 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44422999 168278 0 None 4 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 168278 0 None 4 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL502093 212368 0 None -2 3 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
16154396 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
16197727 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
44285019 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
57514683 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
91898441 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL441738 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
DB04931 299 23 None -5 9 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL370254 210409 3 None 6 4 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 67663 0 None -3 4 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191304 67663 0 None -3 4 Mouse 8.6 pEC50 = 8.6 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL448536 212199 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 96378 0 None -3 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL265236 96378 0 None -3 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
145948876 166911 0 None -5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 166911 0 None -5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
44456964 156137 0 None -1 4 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL406985 156137 0 None -1 4 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL204864 207412 0 None -4 4 Human 6.7 pEC50 = 6.7 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 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 156913 0 None -25 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079298 156913 0 None -25 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL438920 212051 0 None -26 4 Human 6.7 pEC50 = 6.7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 211885 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 211016 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 210475 0 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 169114 0 None -22 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4437801 169114 0 None -22 3 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL320157 209470 0 None 1 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 12129 0 None -21 2 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1184624 12129 0 None -21 2 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL2145456 12129 0 None -21 2 Human 5.7 pEC50 = 5.7 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
46203215 8370 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 428 3 1 3 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1093856 8370 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 428 3 1 3 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1204065 8370 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 428 3 1 3 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44305712 102328 0 None -1 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 421 11 5 3 2.8 NCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305391 102328 0 None -1 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 421 11 5 3 2.8 NCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44359732 28847 0 None -2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 720 19 3 6 2.6 CC(=O)N(CC(=O)N(CC(=O)N(CCCCN=C(N)N)CC(=O)N(CC(N)=O)Cc1cccc2ccccc12)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL138100 28847 0 None -2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 720 19 3 6 2.6 CC(=O)N(CC(=O)N(CC(=O)N(CCCCN=C(N)N)CC(=O)N(CC(N)=O)Cc1cccc2ccccc12)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
164616687 184031 0 None 11 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 13 3 3 5.0 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4849344 184031 0 None 11 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 523 13 3 3 5.0 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL2323793 207764 0 None -27 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 4509 0 None 4 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 4509 0 None 4 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL524861 213837 0 None 3 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 60478 0 None -138 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 60478 0 None -138 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
137639815 156249 0 None -3 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4071063 156249 0 None -3 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
6918780 63122 1 None -204 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
CHEMBL179836 63122 1 None -204 2 Human 6.7 pEC50 = 6.7 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
44347220 167865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 167865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL2370965 208213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 214041 0 None 2 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 184975 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 14 3 3 5.4 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL4863313 184975 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 537 14 3 3 5.4 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL454736 212234 0 None 4 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 212338 2 None -8 7 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 16136 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16136 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44441641 93852 0 None -134 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 93852 0 None -134 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL3350327 209714 0 None -13 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 158859 0 None 2 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932908 158859 0 None 2 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL410091 158859 0 None 2 3 Mouse 5.7 pEC50 = 5.7 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL500516 212336 0 None -1 4 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 195565 0 None -1 4 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568409 195565 0 None -1 4 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
44445083 153759 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 153759 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
164609002 183793 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4845749 183793 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
9808720 63876 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL180892 63876 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
45487287 195962 0 None -3 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL570903 195962 0 None -3 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
46232224 199361 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602654 199361 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487300 195673 0 None -7 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569086 195673 0 None -7 3 Mouse 4.6 pEC50 = 4.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
122184637 121908 0 None -1 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 121908 0 None -1 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
155565321 174993 0 None -7 4 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4579448 174993 0 None -7 4 Mouse 6.6 pEC50 = 6.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44347331 16136 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16136 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL509582 213760 0 None -6 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 13636 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1195347 13636 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL554368 13636 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
15953833 78549 0 None -57 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 5 receptor in cAMP release assayEffective concentration against human melanocortin 5 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 78549 0 None -57 4 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 5 receptor in cAMP release assayEffective concentration against human melanocortin 5 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
155548791 173148 0 None -30 4 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4536340 173148 0 None -30 4 Mouse 5.6 pEC50 = 5.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162670795 182234 0 None -14 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4791112 182234 0 None -14 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
1323 2639 49 None -181 8 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
92432 2639 49 None -181 8 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL430239 2639 49 None -181 8 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
137649368 156852 0 None -35 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4078495 156852 0 None -35 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
44441644 154288 0 None -66 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 154288 0 None -66 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL2310901 207743 0 None -20 4 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 212236 0 None -25 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 97280 0 None -5 5 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL271586 97280 0 None -5 5 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
162654633 180052 0 None -29 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4754987 180052 0 None -29 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
137636060 155678 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4064728 155678 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
44335147 4509 0 None 4 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 4509 0 None 4 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL3350396 209723 0 None -371 4 Human 6.6 pEC50 = 6.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 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 210495 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 207761 0 None -8 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 158022 0 None -3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4091894 158022 0 None -3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155567887 175464 0 None -1 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4590532 175464 0 None -1 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL263878 208843 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 209649 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 12654 0 None -41 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 12654 0 None -41 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL3216179 12654 0 None -41 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
1338 3735 37 None -257 7 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 3735 37 None -257 7 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 3735 37 None -257 7 Human 5.6 pEC50 = 5.6 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
155545201 172865 0 None -1 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 602 14 6 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4529287 172865 0 None -1 2 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 602 14 6 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
10864861 114689 2 None -128 2 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1 10.1021/jm025539h
CHEMBL334457 114689 2 None -128 2 Human 6.6 pEC50 = 6.6 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1 10.1021/jm025539h
45487411 195359 0 None -10 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567240 195359 0 None -10 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL266417 208928 0 None -776 6 Human 7.6 pEC50 = 7.6 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 208211 0 None 85 2 Human 7.6 pEC50 = 7.6 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 96462 0 None -46 4 Human 6.6 pEC50 = 6.6 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 96462 0 None -46 4 Human 6.6 pEC50 = 6.6 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
10257242 14846 0 None -42 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 14846 0 None -42 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL430843 211863 0 None 2 3 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 120731 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 998 10 10 10 0.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)c2cc3ccccc3cc2NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577992 120731 0 None -2 2 Mouse 4.6 pEC50 = 4.6 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
ChEMBL 998 10 10 10 0.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)c2cc3ccccc3cc2NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
155554244 174367 0 None -15 3 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4565607 174367 0 None -15 3 Mouse 4.6 pEC50 = 4.6 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44305763 201388 0 None -1 4 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL63850 201388 0 None -1 4 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL2323786 207757 0 None -2 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)
ChEMBL 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 156984 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4080138 156984 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
46232222 199360 0 None -4 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602653 199360 0 None -4 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
44441648 154141 0 None -41 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 154141 0 None -41 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137635422 155357 0 None -72 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 155357 0 None -72 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL264190 208853 1 None 2 8 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 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 111240 0 None -1 5 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111240 0 None -1 5 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155544214 172749 0 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 172749 0 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173295 0 None -7 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539621 173295 0 None -7 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155550083 173332 0 None 5 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4540411 173332 0 None 5 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
11308957 69035 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL193151 69035 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL264190 208853 1 None 2 8 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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 139206 0 None 1 5 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
132991507 139206 0 None 1 5 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798421 139206 0 None 1 5 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL439128 212067 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 209811 0 None -7 4 Mouse 8.5 pEC50 = 8.5 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 208853 1 None 2 8 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
1323 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
1323 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
1323 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
1323 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
1323 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2639 49 None -181 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL393075 210705 0 None -20 4 Human 8.5 pEC50 = 8.5 Functional
Effect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 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 132593 0 None -5 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL370261 132593 0 None -5 4 Mouse 8.5 pEC50 = 8.5 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
155564058 174752 0 None -16 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4574056 174752 0 None -16 4 Mouse 8.5 pEC50 = 8.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL264190 208853 1 None 2 8 Mouse 8.5 pEC50 = 8.5 Functional
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 182567 0 None -15 3 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4795352 182567 0 None -15 3 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL2370964 208212 0 None -10 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 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 211837 0 None 2 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 208212 0 None -10 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 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 208853 1 None -3 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 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
127047913 139381 0 None 4 5 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799563 139381 0 None 4 5 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL264190 208853 1 None 2 8 Mouse 8.4 pEC50 = 8.4 Functional
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 184801 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860714 184801 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL510687 213801 0 None -3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 173915 0 None 1 4 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4554828 173915 0 None 1 4 Mouse 7.5 pEC50 = 7.5 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL203602 207406 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 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 171042 0 None 1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4465466 171042 0 None 1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44401530 12671 0 None -51 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1188092 12671 0 None -51 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL535152 12671 0 None -51 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
44347119 113911 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 113911 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
45487405 195751 0 None -25 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 587 16 8 6 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569695 195751 0 None -25 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 587 16 8 6 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
51350673 58477 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53317148 58477 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932362 58477 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688104 58477 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
44305790 102354 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305559 102354 0 None -1 3 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
45487294 195128 0 None -3 4 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565688 195128 0 None -3 4 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2371973 208415 0 None 57 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 180943 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4765199 180943 0 None 2 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
162664463 181598 0 None 4 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4782762 181598 0 None 4 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
46232223 197475 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589468 197475 0 None -1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 9 8 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL302703 209159 0 None 5 5 Mouse 6.5 pEC50 = 6.5 Functional
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 199328 0 None 3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602299 199328 0 None 3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
44456958 96941 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
CHEMBL269837 96941 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
CHEMBL104880 206713 0 None 1 2 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 201637 0 None -1 4 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL64954 201637 0 None -1 4 Mouse 4.5 pEC50 = 4.5 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44275650 93607 0 None -83 4 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 93607 0 None -83 4 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
1323 2639 49 None -181 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
92432 2639 49 None -181 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL430239 2639 49 None -181 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
137645483 157064 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 906 11 11 10 -1.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4081092 157064 0 None 1 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 906 11 11 10 -1.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
44391927 13863 0 None -66 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 13863 0 None -66 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL3216393 13863 0 None -66 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
53318436 58480 0 None -2 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
CHEMBL1688108 58480 0 None -2 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
CHEMBL103817 206707 0 None -2 4 Mouse 7.5 pEC50 = 7.5 Functional
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 140124 0 None -117 4 Human 6.5 pEC50 = 6.5 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 140124 0 None -117 4 Human 6.5 pEC50 = 6.5 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
137658359 159012 0 None -6 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102774 159012 0 None -6 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL488355 212294 0 None -3 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 184962 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4863206 184962 0 None -1 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
44401522 12660 0 None -97 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1188041 12660 0 None -97 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL534928 12660 0 None -97 2 Human 6.5 pEC50 = 6.5 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
44391938 11626 0 None -20 2 Human 6.5 pEC50 = 6.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1181567 11626 0 None -20 2 Human 6.5 pEC50 = 6.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL2145455 11626 0 None -20 2 Human 6.5 pEC50 = 6.5 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
45487417 195358 0 None -8 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL567233 195358 0 None -8 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL602650 214030 0 None 2 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 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 210796 15 None -22 7 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 210796 15 None -22 7 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 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 207524 31 None -81 8 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 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 207770 0 None -22 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 199387 0 None 4 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602852 199387 0 None 4 3 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
46885761 7931 0 None -56 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL1090813 7931 0 None -56 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL441988 212147 2 None 162 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 181589 0 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4782693 181589 0 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL389674 210676 0 None 1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 207524 31 None -81 8 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 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 207524 31 None -81 8 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 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 207524 31 None -81 8 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 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 207524 31 None -81 8 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 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 207002 0 None -1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 13861 0 None -61 2 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1196956 13861 0 None -61 2 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL558787 13861 0 None -61 2 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 599 7 4 5 3.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1 10.1016/j.bmcl.2005.02.068
44408253 139801 0 None -141 4 Human 5.4 pEC50 = 5.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 139801 0 None -141 4 Human 5.4 pEC50 = 5.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
46885712 7973 0 None -204 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 7973 0 None -204 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1204061 7973 0 None -204 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL104052 206710 0 None -1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 8020 0 None -52 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1091631 8020 0 None -52 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
145980719 165932 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 165932 0 None 1 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44448660 94519 0 None -52 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 94519 0 None -52 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
137637656 155685 0 None -40 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 155685 0 None -40 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
164626210 185898 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 670 12 4 4 7.0 CC[C@H](C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccc(O)cc1)N1C[C@@H](Cc2ccccc2)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4877184 185898 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 670 12 4 4 7.0 CC[C@H](C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccc(O)cc1)N1C[C@@H](Cc2ccccc2)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44441643 154250 0 None -43 2 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400252 154250 0 None -43 2 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44347927 156722 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 156722 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
162662213 180904 0 None 2 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4764827 180904 0 None 2 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
44457043 97150 0 None -3 5 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL270923 97150 0 None -3 5 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
51350799 58478 0 None 3 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53323763 58478 0 None 3 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932356 58478 0 None 3 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688105 58478 0 None 3 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
1334 1468 6 None -17 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1468 6 None -17 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1468 6 None -17 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44310243 168610 0 None 2 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932909 168610 0 None 2 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL440633 168610 0 None 2 3 Mouse 5.4 pEC50 = 5.4 Functional
Effective concentration against mouse Melanocortin 5 receptorEffective concentration against mouse Melanocortin 5 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
46232221 197480 0 None -1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589516 197480 0 None -1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
44305805 100402 0 None 1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 393 9 5 3 2.0 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL293673 100402 0 None 1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 393 9 5 3 2.0 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL264190 208853 1 None 2 8 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 139450 0 None 4 5 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799955 139450 0 None 4 5 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL264190 208853 1 None 2 8 Mouse 8.4 pEC50 = 8.4 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 172307 0 None -1 4 Mouse 8.4 pEC50 = 8.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4515666 172307 0 None -1 4 Mouse 8.4 pEC50 = 8.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL2370968 208216 0 None -1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 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 208216 0 None -1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC5R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 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 208853 1 None 2 8 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 210594 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 210823 0 None 1 4 Mouse 8.4 pEC50 = 8.4 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 67263 0 None -4 4 Mouse 8.4 pEC50 = 8.4 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL190366 67263 0 None -4 4 Mouse 8.4 pEC50 = 8.4 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
155567399 175383 0 None 17 4 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4588429 175383 0 None 17 4 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
11181928 165593 0 None -1 4 Mouse 8.3 pEC50 = 8.3 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL426282 165593 0 None -1 4 Mouse 8.3 pEC50 = 8.3 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3799094 210511 0 None 8 5 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 157735 0 None 3 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4088980 157735 0 None 3 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
155542040 172499 0 None -199 4 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4519837 172499 0 None -199 4 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155549865 173274 0 None 10 4 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539175 173274 0 None 10 4 Mouse 7.4 pEC50 = 7.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
44408287 75021 0 None -162 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75021 0 None -162 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44408275 75053 0 None -47 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75053 0 None -47 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL3287060 209543 0 None -6 5 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 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 209444 0 None 3 4 Mouse 5.4 pEC50 = 5.4 Functional
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 174178 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 656 13 5 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4561005 174178 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 656 13 5 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL2096759 207454 0 None -23 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 156449 0 None -56 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4073316 156449 0 None -56 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
118735100 118282 0 None -91 4 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 118282 0 None -91 4 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL104010 206709 0 None -1 2 Mouse 4.4 pEC50 = 4.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207760 0 None -213 4 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 208115 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 175151 0 None -13 3 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582914 175151 0 None -13 3 Mouse 5.4 pEC50 = 5.4 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL106959 206722 0 None -2 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 166716 0 None -25 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 166716 0 None -25 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44457002 97110 0 None 1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
CHEMBL270691 97110 0 None 1 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
44577510 188139 0 None -33 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188139 0 None -33 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
164627532 186016 0 None 18 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 11 3 3 6.1 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4878922 186016 0 None 18 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 11 3 3 6.1 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
137657607 159077 0 None -81 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103567 159077 0 None -81 3 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
122184576 121900 0 None -32 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 121900 0 None -32 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44401313 12166 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1184856 12166 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL2028956 12166 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
11273288 12836 0 None -181 3 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 12836 0 None -181 3 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL538567 12836 0 None -181 3 Human 6.4 pEC50 = 6.4 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL410168 211047 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 94614 0 None -47 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 94614 0 None -47 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP releaseAgonist activity at human MC5R expressed in CHO cells assesses as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
102096778 58483 0 None -5 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
51351277 58483 0 None -5 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
53322400 58483 0 None -5 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
91932360 58483 0 None -5 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL1688111 58483 0 None -5 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2323794 207765 0 None -5 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 156274 0 None 2 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4071283 156274 0 None 2 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL2372365 208469 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 168302 0 None -32 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168302 0 None -32 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL3600840 210060 0 None -1 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 207769 0 None -15 4 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 207730 0 None -2 4 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL 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 184676 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 12 3 3 6.9 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4858724 184676 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 12 3 3 6.9 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
45487285 195308 0 None -7 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 627 15 9 7 0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2cc(O)ccc2c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566760 195308 0 None -7 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 627 15 9 7 0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2cc(O)ccc2c1)C(N)=O 10.1016/j.bmcl.2009.07.025
168295131 191634 0 None -7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 191634 0 None -7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
137654884 158039 0 None 3 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4092082 158039 0 None 3 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
44408252 140125 0 None -30 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140125 0 None -30 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
164621683 185001 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 12 3 3 6.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4863711 185001 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 12 3 3 6.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
44441636 93565 0 None -6 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248701 93565 0 None -6 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
46232227 197481 0 None 2 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589517 197481 0 None 2 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL3349030 209649 0 None -8 3 Human 7.3 pEC50 = 7.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 14855 0 None -16 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 14855 0 None -16 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC5 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
164624386 185606 0 None -1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185606 0 None -1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 211398 0 None -83 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
16133814 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm000211e
71457994 78154 0 None -12 4 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
CHEMBL2112213 78154 0 None -12 4 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
44305770 201097 0 None -2 4 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL62228 201097 0 None -2 4 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
155542149 172512 0 None -2 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 172512 0 None -2 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173739 0 None -2 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173739 0 None -2 3 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 174709 0 None -16 4 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4572994 174709 0 None -16 4 Mouse 8.3 pEC50 = 8.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
118722929 115719 0 None -6 4 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358538 115719 0 None -6 4 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3287329 209555 0 None -1 5 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 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 212385 0 None 1 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 115716 0 None -7 4 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358534 115716 0 None -7 4 Mouse 8.3 pEC50 = 8.3 Functional
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
122179552 120960 0 None 2 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
CHEMBL3582446 120960 0 None 2 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
162661397 180934 0 None 1 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4765156 180934 0 None 1 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
1323 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
162649653 179510 0 None -9 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4748317 179510 0 None -9 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
1323 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
92432 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
CHEMBL438294 212008 0 None 5 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 173029 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173029 0 None 6 3 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 173966 0 None -165 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4556149 173966 0 None -165 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155560756 174503 0 None 5 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4568647 174503 0 None 5 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
132180599 156339 0 None -3 4 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4072129 156339 0 None -3 4 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
164618352 184054 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 11 3 3 6.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4849626 184054 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 608 11 3 3 6.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
137657385 159207 0 None - 1 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4105142 159207 0 None - 1 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL2112008 207472 0 None -14 3 Human 5.3 pEC50 = 5.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 212246 0 None 1 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 209476 0 None 5 4 Mouse 7.3 pEC50 = 7.3 Functional
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 185902 0 None -1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185902 0 None -1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 12154 0 None -19 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 607 9 3 5 3.5 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1184771 12154 0 None -19 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 607 9 3 5 3.5 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL2145454 12154 0 None -19 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 607 9 3 5 3.5 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1 10.1016/j.bmcl.2004.10.020
46885711 7972 0 None -169 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 7972 0 None -169 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL2323785 207756 0 None -8 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 175513 0 None -87 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4591394 175513 0 None -87 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4299612 211836 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 155746 0 None -3 6 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 155746 0 None -3 6 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
44441647 154140 0 None -22 3 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399714 154140 0 None -22 3 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
164609537 183805 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 12 3 3 7.6 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4845842 183805 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 12 3 3 7.6 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
164623182 185027 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185027 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 31844 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 699 19 8 7 -0.2 CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
CHEMBL140847 31844 0 None 1 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 699 19 8 7 -0.2 CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
44347219 16388 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 16388 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
44359580 32643 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 713 20 5 7 0.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL141497 32643 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 713 20 5 7 0.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
164621263 184890 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 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 184890 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 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 158997 0 None -11 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102613 158997 0 None -11 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155549385 173223 0 None 4 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4538225 173223 0 None 4 4 Mouse 7.3 pEC50 = 7.3 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162662360 180879 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4764556 180879 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse MC5R by alphascreen cAMP assayAgonist activity at mouse MC5R by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
1334 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL410795 211085 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
16133814 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1468 6 None -17 4 Human 6.3 pEC50 = 6.3 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
137657206 159112 0 None -2 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103985 159112 0 None -2 3 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL421028 211504 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 207000 0 None 8 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 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 163742 0 None -138 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 163742 0 None -138 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
164613550 184536 0 None 12 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4856539 184536 0 None 12 3 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
164625589 185149 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 11 3 3 7.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4866151 185149 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 612 11 3 3 7.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44445082 153756 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 153756 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
137659091 158781 0 None -6 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4100160 158781 0 None -6 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
164615813 184551 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of 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 184551 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of 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 185999 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of 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 185999 0 None -1 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of 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 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2639 49 None -181 8 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL2115441 207514 0 None -64 4 Human 8.2 pEC50 = 8.2 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor
ChEMBL 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 207348 0 None -2 4 Mouse 8.2 pEC50 = 8.2 Functional
In vitro agonist potency for Mouse Melanocortin 5 receptorIn vitro agonist potency for Mouse Melanocortin 5 receptor
ChEMBL 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
16132144 207524 31 None -1 8 Mouse 8.2 pEC50 = 8.2 Functional
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 207524 31 None -1 8 Mouse 8.2 pEC50 = 8.2 Functional
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 207524 31 None -1 8 Mouse 8.2 pEC50 = 8.2 Functional
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 207524 31 None -1 8 Mouse 8.2 pEC50 = 8.2 Functional
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 121865 0 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 121865 0 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 183835 0 None -3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 183835 0 None -3 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 184126 0 None 47 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4850501 184126 0 None 47 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
155561730 175070 0 None -19 3 Mouse 6.2 pEC50 = 6.2 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4581269 175070 0 None -19 3 Mouse 6.2 pEC50 = 6.2 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
137637251 155353 0 None -6 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 820 10 9 8 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4060767 155353 0 None -6 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 820 10 9 8 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL433296 211878 0 None 1 4 Mouse 7.2 pEC50 = 7.2 Functional
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 185498 0 None 2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4871577 185498 0 None 2 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
45487286 195655 0 None -10 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568940 195655 0 None -10 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL3600922 210068 0 None 2 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 75141 0 None -61 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75141 0 None -61 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
45487298 195656 0 None -7 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568965 195656 0 None -7 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2323800 207771 0 None -39 4 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 184843 0 None 11 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 545 13 4 4 4.7 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4861482 184843 0 None 11 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 545 13 4 4 4.7 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
44441639 93603 0 None -11 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248893 93603 0 None -11 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL105113 206714 0 None 1 4 Mouse 6.2 pEC50 = 6.2 Functional
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 158820 0 None -99 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 158820 0 None -99 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
45487409 195212 0 None -9 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566162 195212 0 None -9 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44441633 94081 0 None -18 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL251735 94081 0 None -18 2 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
46885907 7943 0 None -104 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1090885 7943 0 None -104 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
44408173 75036 0 None -154 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75036 0 None -154 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
164621924 185359 0 None 6 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185359 0 None 6 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185911 0 None -3 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4877442 185911 0 None -3 3 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
44441642 153859 0 None -75 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 153859 0 None -75 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487418 195555 0 None -8 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 632 17 8 8 0.0 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568341 195555 0 None -8 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 632 17 8 8 0.0 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL227239 207696 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 157340 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084136 157340 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
45487410 195752 0 None -21 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569696 195752 0 None -21 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
137642664 157523 0 None -7 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4086346 157523 0 None -7 3 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL320157 209470 0 None 1 4 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 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 156485 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 858 19 8 6 2.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4073782 156485 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 858 19 8 6 2.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
45487297 195415 0 None -13 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567634 195415 0 None -13 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44441645 93680 0 None -63 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 93680 0 None -63 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
45487406 195209 0 None -6 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566150 195209 0 None -6 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL65339 214073 0 None 1 3 Mouse 5.2 pEC50 = 5.2 Functional
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 208516 0 None -691 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 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 207759 0 None -13 4 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 195595 0 None -6 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568577 195595 0 None -6 4 Mouse 5.2 pEC50 = 5.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
137644603 157593 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 848 19 9 7 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4087277 157593 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 848 19 9 7 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL322889 209479 0 None 3 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 210055 0 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 157328 0 None -1 5 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL408398 157328 0 None -1 5 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cellsAgonist activity at mouse MC5R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL322610 209478 0 None 2 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 212356 0 None -2 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 182498 0 None -16 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 182498 0 None -16 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL50056 212338 2 None -8 7 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 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 159070 0 None 6 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 868 10 10 9 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4103508 159070 0 None 6 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 868 10 10 9 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
45487290 195095 0 None -22 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565474 195095 0 None -22 3 Mouse 4.2 pEC50 = 4.2 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
44401520 13802 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1196472 13802 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL557154 13802 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 571 8 4 5 3.3 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
137661461 158817 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4100584 158817 0 None - 1 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
51351151 58482 0 None -2 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318437 58482 0 None -2 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932359 58482 0 None -2 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688110 58482 0 None -2 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
137632394 155726 0 None - 1 Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4065189 155726 0 None - 1 Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
145948912 166913 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 166913 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
122179551 120959 0 None -1 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL3582445 120959 0 None -1 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL2370533 208113 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 206714 0 None 1 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Evaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC5R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3735 37 None -257 7 Human 6.1 pEC50 = 6.1 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC5R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44359589 31249 0 None 3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL140324 31249 0 None 3 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL438235 212001 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 185182 0 None -1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4866532 185182 0 None -1 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL104397 206711 0 None 2 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 174588 0 None -6 3 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4570356 174588 0 None -6 3 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
137656521 159185 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 159185 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44401524 13877 0 None -120 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 583 8 4 5 3.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1197052 13877 0 None -120 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 583 8 4 5 3.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL559181 13877 0 None -120 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 583 8 4 5 3.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL227833 207697 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 209649 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 207763 0 None -1 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 139255 0 None -74 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798768 139255 0 None -74 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
10122170 129784 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 638 10 3 7 2.2 CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL368008 129784 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Effective concentration determined against melanocortin-5 receptorEffective concentration determined against melanocortin-5 receptor
ChEMBL 638 10 3 7 2.2 CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
1323 2639 49 None -181 8 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2639 49 None -181 8 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2639 49 None -181 8 Human 8.1 pEC50 = 8.1 Functional
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
155556466 173834 0 None -11 4 Mouse 8.1 pEC50 = 8.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4552764 173834 0 None -11 4 Mouse 8.1 pEC50 = 8.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL501679 212362 0 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL 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 199388 0 None 6 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602853 199388 0 None 6 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589308 214012 0 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 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 207524 31 None -81 8 Human 8.1 pEC50 = 8.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 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 211421 0 None 5 5 Mouse 8.1 pEC50 = 8.1 Functional
Maximum agonist response for mouse melanocortin 5 receptor (MC5R)Maximum agonist response for mouse melanocortin 5 receptor (MC5R)
ChEMBL 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 157295 0 None -16 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4083717 157295 0 None -16 4 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
155562237 175126 0 None -39 4 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582276 175126 0 None -39 4 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44408155 140010 0 None -114 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140010 0 None -114 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
164622957 185522 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4871777 185522 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164627764 185972 0 None -2 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 185972 0 None -2 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 209649 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 122030 0 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 122030 0 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 210487 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC5R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 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 210796 15 None -109 7 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 210796 15 None -109 7 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 211122 0 None -4 4 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 210796 15 None -109 7 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 210796 15 None -109 7 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor
ChEMBL 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 173360 0 None -38 4 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4541098 173360 0 None -38 4 Mouse 6.1 pEC50 = 6.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44305956 102275 0 None -2 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL305132 102275 0 None -2 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
44305784 201639 0 None -1 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 201639 0 None -1 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
ChEMBL 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 207758 0 None -41 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 155484 0 None -1 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4062425 155484 0 None -1 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL3600921 210067 0 None -6 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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 12291 0 None -25 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 571 8 3 5 3.3 CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1185810 12291 0 None -25 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 571 8 3 5 3.3 CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL2145453 12291 0 None -25 2 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
ChEMBL 571 8 3 5 3.3 CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL502300 212371 0 None -6 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 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 210535 0 None 4 3 Human 6.1 pEC50 = 6.1 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 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 140818 0 None -218 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 140818 0 None -218 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC5R by cAMP accumulationActivity against human MC5R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL2323797 207768 0 None -44 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 3357 4 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3357 4 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3357 4 None -3 4 Human 6.1 pEC50 = 6.1 Functional
Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
10188529 126247 0 None -34 3 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 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 126247 0 None -34 3 Human 6.1 pEC50 = 6.1 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 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 195167 0 None -4 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 628 16 9 8 -0.3 N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565900 195167 0 None -4 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 628 16 9 8 -0.3 N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL2323796 207767 0 None -79 3 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 97030 0 None -1 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL270270 97030 0 None -1 4 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL331259 209605 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.Increase in intracellular cAMP in CHO cells expressing human melanocortin receptor 5.
ChEMBL 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 210963 0 None 2 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 12661 0 None -125 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 557 7 4 5 2.9 C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1188043 12661 0 None -125 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 557 7 4 5 2.9 C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL534930 12661 0 None -125 2 Human 6.1 pEC50 = 6.1 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 557 7 4 5 2.9 C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
71456219 78322 0 None -23 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 78322 0 None -23 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)Effective concentration of peptide at 50% maximal cAMP generation (10e-10 to 10e-4 M)
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44441684 93684 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 93684 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
162672755 182498 0 None -16 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 182498 0 None -16 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL2323795 207766 0 None -19 4 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 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 208853 1 None 2 8 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 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 207873 0 None -1 4 Mouse 7.1 pEC50 = 7.1 Functional
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 173221 0 None 1 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4538209 173221 0 None 1 3 Mouse 7.1 pEC50 = 7.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155554827 174037 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4557656 174037 0 None -2 3 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155562993 174649 0 None 1 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 694 14 6 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4571760 174649 0 None 1 2 Mouse 5.1 pEC50 = 5.1 Functional
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayFull agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 694 14 6 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137637026 155372 0 None -162 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 155372 0 None -162 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44401321 11676 0 None -19 2 Human 6.0 pEC50 = 6.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL1181867 11676 0 None -19 2 Human 6.0 pEC50 = 6.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
CHEMBL2028960 11676 0 None -19 2 Human 6.0 pEC50 = 6.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
ChEMBL 597 8 4 5 3.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1 10.1016/j.bmcl.2005.02.068
102096778 58483 0 None -5 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351277 58483 0 None -5 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322400 58483 0 None -5 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932360 58483 0 None -5 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688111 58483 0 None -5 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
45487415 195753 0 None -11 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569697 195753 0 None -11 4 Mouse 6.0 pEC50 = 6.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
164625186 185375 0 None 2 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4869669 185375 0 None 2 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
145973975 164094 0 None -22 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164094 0 None -22 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
46885480 7657 0 None -63 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 7657 0 None -63 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assayAgonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
45487412 195138 0 None -8 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565740 195138 0 None -8 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonistic activity against mouse MC5RAgonistic activity against mouse MC5R
ChEMBL 605 17 9 7 -0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL430489 211862 0 None 2 3 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)
ChEMBL 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 93682 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 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 93682 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human MC5R assessed as stimulation of cAMP productionAntagonist activity at human MC5R assessed as stimulation of cAMP production
ChEMBL 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 212090 0 None -16 3 Human 7.0 pEC50 = 7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 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 211986 0 None -63 3 Human 7.0 pEC50 = 7 Functional
Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.
ChEMBL 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 58479 0 None -4 4 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318435 58479 0 None -4 4 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932358 58479 0 None -4 4 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688106 58479 0 None -4 4 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
168277916 190073 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5181812 190073 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168290510 191290 0 None -1288 4 Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 191290 0 None -1288 4 Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168293710 191558 0 None -1288 4 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 191558 0 None -1288 4 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168278271 190511 0 None -2818 4 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 190511 0 None -2818 4 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168276507 189661 0 None -1584 4 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 189661 0 None -1584 4 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168285101 191038 0 None -7079 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191038 0 None -7079 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168273645 189721 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5176443 189721 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168271237 189884 0 None -6760 4 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 189884 0 None -6760 4 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168285904 191064 0 None -10232 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 191064 0 None -10232 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168294114 191582 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5204285 191582 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168274920 189659 0 None -6025 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 189659 0 None -6025 4 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168283616 190635 0 None -331 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 190635 0 None -331 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
11993702 3523 18 None -12589 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3523 18 None -12589 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3523 18 None -12589 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3523 18 None -12589 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3523 18 None -12589 4 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
168272660 189829 0 None -1548 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 189829 0 None -1548 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168277543 190071 0 None -4897 4 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 190071 0 None -4897 4 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
10408 711 26 None -467 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 711 26 None -467 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 711 26 None -467 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 711 26 None -467 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 711 26 None -467 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 190776 0 None -1047 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 190776 0 None -1047 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168272615 189783 0 None -4073 4 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 189783 0 None -4073 4 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168284256 190342 0 None -4570 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 190342 0 None -4570 4 Human 6.7 pIC50 = 6.7 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168271934 189482 0 None -288 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 189482 0 None -288 4 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 191867 0 None -13489 4 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 191867 0 None -13489 4 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168270124 189352 0 None -1819 4 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 189352 0 None -1819 4 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1323 2639 49 None -181 8 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2639 49 None -181 8 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2639 49 None -181 8 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
168276294 189904 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179373 189904 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168284733 191018 0 None -162 4 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 191018 0 None -162 4 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289404 190708 0 None -933 4 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 190708 0 None -933 4 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168277258 190106 0 None -870 4 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 190106 0 None -870 4 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168281389 190318 0 None -218 4 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 190318 0 None -218 4 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
168277761 189696 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175981 189696 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168295726 191797 0 None -9120 4 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 191797 0 None -9120 4 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168281421 190353 0 None -794 3 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 190353 0 None -794 3 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL413573 211317 0 None -1 4 Human 8.7 pKd = 8.7 Functional
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 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 96614 0 None -1 4 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 96614 0 None -1 4 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
132938008 158954 0 None -891 5 Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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 158954 0 None -891 5 Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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 174391 0 None -269 5 Mouse 6.5 pKd = 6.5 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 174391 0 None -269 5 Mouse 6.5 pKd = 6.5 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
122184635 121906 0 None 2 4 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 121906 0 None 2 4 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC5 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
162650385 179481 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4747952 179481 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL3577981 209992 1 None -177 5 Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 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
CHEMBL3577981 209992 1 None -177 5 Mouse 6.4 pKd = 6.4 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 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 188410 0 None -2 2 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 188410 0 None -2 2 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human melanocortin 5 receptor expressed in HEK293 cellsAntagonist activity at human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
132938008 158954 0 None -891 5 Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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 158954 0 None -891 5 Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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
155544852 174357 0 None -331 5 Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 174357 0 None -331 5 Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
162645080 178860 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4740561 178860 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
155548853 173227 0 None -758 5 Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 173227 0 None -758 5 Mouse 6.1 pKd = 6.1 Functional
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
131839615 210879 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 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 210879 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 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 210879 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
Drug Central 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 210879 20 None 1 7 Human 8.1 pIC50 = 8.1 Functional
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 210879 20 None 1 7 Human 8.1 pIC50 = 8.1 Functional
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 210879 20 None 1 7 Human 8.1 pIC50 = 8.1 Functional
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 3015 0 None 6 3 Human 10.5 pIC50 None 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1335 312 0 None -630 3 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9892020
1342 245 0 None - 1 Human 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12904077
1324 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16154396 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16197727 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
44285019 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
57514683 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
91898441 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL441738 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
DB04931 299 23 None -14 9 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1323 2639 49 None -181 8 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
92432 2639 49 None -181 8 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL430239 2639 49 None -181 8 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44366081 10150 0 None - 2 Human 10.5 pEC50 = 10.5 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10150 0 None - 2 Human 10.5 pEC50 = 10.5 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
1323 2639 49 None - 3 Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
92432 2639 49 None - 3 Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL430239 2639 49 None - 3 Mouse 10.2 pEC50 = 10.2 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16154396 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44285019 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
57514683 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
91898441 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL441738 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
DB04931 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
1324 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
16154396 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
44285019 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
57514683 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
91898441 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
CHEMBL441738 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
DB04931 299 23 None - 4 Mouse 10.2 pEC50 = 10.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL None None None None 10.1021/jm0104872
CHEMBL1161322 206756 0 None - 2 Human 10.1 pEC50 = 10.1 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
16154396 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
44285019 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
57514683 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
91898441 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL441738 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
DB04931 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
Effective concentration for mouse Melanocortin-5 receptorEffective concentration for mouse Melanocortin-5 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL2096742 207452 0 None - 2 Human 9.9 pEC50 = 9.9 Binding
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 212158 0 None -1 3 Human 9.9 pEC50 = 9.9 Binding
Signal transduction efficacy in cAMP assay in CHO cells expressing human melanocortin receptor 5Signal transduction efficacy in cAMP assay in CHO cells expressing human melanocortin receptor 5
ChEMBL 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 2639 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
92432 2639 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL430239 2639 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44327392 141319 0 None - 0 Mouse 9.8 pEC50 = 9.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1025 21 12 12 -0.6 CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0104872
CHEMBL386583 141319 0 None - 0 Mouse 9.8 pEC50 = 9.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 1025 21 12 12 -0.6 CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0104872
CHEMBL1161323 206757 0 None - 2 Human 9.7 pEC50 = 9.7 Binding
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 207524 31 None - 4 Mouse 9.5 pEC50 = 9.5 Binding
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 207524 31 None - 4 Mouse 9.5 pEC50 = 9.5 Binding
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 207524 31 None - 4 Mouse 9.5 pEC50 = 9.5 Binding
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 207524 31 None - 4 Mouse 9.5 pEC50 = 9.5 Binding
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 207985 0 None - 0 Mouse 9.4 pEC50 = 9.4 Binding
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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 207524 31 None - 4 Mouse 9.4 pEC50 = 9.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 207993 0 None - 0 Mouse 9.3 pEC50 = 9.3 Binding
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 2639 49 None - 3 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
92432 2639 49 None - 3 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL430239 2639 49 None - 3 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL2369964 207990 0 None - 0 Mouse 9.0 pEC50 = 9.0 Binding
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 105515 0 None -4 3 Human 9.0 pEC50 = 9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 105515 0 None -4 3 Human 9.0 pEC50 = 9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL2369963 207989 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
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 206753 0 None - 2 Human 8.0 pEC50 = 8 Binding
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 209956 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207325 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210284 0 None - 0 Mouse 6.0 pEC50 = 6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 171304 0 None - 0 Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL446941 171304 0 None - 0 Human 5.0 pEC50 = 5 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
10260053 167629 0 None -6 3 Human 6.0 pEC50 = 6.0 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 167629 0 None -6 3 Human 6.0 pEC50 = 6.0 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL347216 209955 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207308 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 209066 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 211873 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 200123 0 None -5 3 Human 5.9 pEC50 = 5.9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 200123 0 None -5 3 Human 5.9 pEC50 = 5.9 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL94391 214122 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 209538 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 211883 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207312 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 209959 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 167482 0 None -11 3 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 167482 0 None -11 3 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL1161321 206755 0 None - 2 Human 7.8 pEC50 = 7.8 Binding
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 208262 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 209914 0 None - 1 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 118363 0 None - 2 Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422433 118363 0 None - 2 Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL190953 207323 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210415 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208518 0 None - 2 Human 8.7 pEC50 = 8.7 Binding
Activity of cyclic alpha MSH analogues at human melanocortin receptor Melanocortin 5 receptorActivity of cyclic alpha MSH analogues at human melanocortin receptor Melanocortin 5 receptor
ChEMBL 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
CHEMBL2369969 207995 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
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 207452 0 None - 2 Mouse 8.6 pEC50 = 8.6 Binding
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 207999 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
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 3530 12 None - 7 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
6440621 3530 12 None - 7 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
9898183 3530 12 None - 7 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL3422426 3530 12 None - 7 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
118735609 118362 0 None - 2 Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422432 118362 0 None - 2 Mouse 4.7 pEC50 = 4.7 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
44269217 30031 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL13910 30031 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL2369974 208000 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
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 209561 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 118361 0 None - 1 Mouse 4.6 pEC50 = 4.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 877 18 9 7 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL3422429 118361 0 None - 1 Mouse 4.6 pEC50 = 4.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 877 18 9 7 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/ml500340z
11828678 206127 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 721 16 8 6 1.0 CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm0104872
CHEMBL96531 206127 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 721 16 8 6 1.0 CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm0104872
CHEMBL2096745 207453 0 None - 0 Mouse 4.6 pEC50 = 4.6 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207326 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210410 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 98029 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276012 98029 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
118735604 118359 0 None - 2 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL3422427 118359 0 None - 2 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL329847 209565 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 208008 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
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 207986 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
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 208046 0 None -6 3 Human 8.5 pEC50 = 8.5 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 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 207991 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
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 44976 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL152612 44976 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL264190 208853 1 None - 2 Mouse 8.4 pEC50 = 8.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 209575 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 210286 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207305 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207307 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208002 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
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 207048 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 208853 1 None - 2 Mouse 7.5 pEC50 = 7.5 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 209965 0 None - 0 Mouse 4.4 pEC50 = 4.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 214134 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 211864 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 208263 0 None - 0 Mouse 4.4 pEC50 = 4.4 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 206754 0 None - 2 Human 6.4 pEC50 = 6.4 Binding
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 97873 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL275067 97873 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL190203 207310 0 None - 0 Mouse 5.4 pEC50 = 5.4 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208853 1 None - 2 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 209986 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 208009 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
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 209577 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 209452 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 161363 0 None -208 3 Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 161363 0 None -208 3 Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 161363 0 None -208 3 Human 7.4 pEC50 = 7.4 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL2369966 207992 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
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 207987 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
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 38238 13 None - 0 Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
CHEMBL14642 38238 13 None - 0 Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 559 12 2 7 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1 10.1021/jm025600i
CHEMBL1161316 206752 0 None - 2 Human 7.4 pEC50 = 7.4 Binding
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 155150 0 None - 1 Mouse 7.3 pEC50 = 7.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL405174 155150 0 None - 1 Mouse 7.3 pEC50 = 7.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL151906 207042 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207049 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 208001 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
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 207996 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
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 208380 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 211875 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 120768 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 120768 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL3422430 209913 0 None - 1 Mouse 5.3 pEC50 = 5.3 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 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 205189 0 None -114 3 Human 6.3 pEC50 = 6.3 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 205189 0 None -114 3 Human 6.3 pEC50 = 6.3 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL94369 214121 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 208382 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207300 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208379 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208381 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 168419 0 None -741 3 Human 6.2 pEC50 = 6.2 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 168419 0 None -741 3 Human 6.2 pEC50 = 6.2 Binding
Effective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cellsEffective concentration against human melanocortin 5 receptor (hMC5R) in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL320157 209470 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 207994 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
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 207997 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
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 207450 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207988 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
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 207043 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 210046 0 None - 0 Mouse 5.1 pEC50 = 5.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 209954 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 118360 0 None - 1 Mouse 5.1 pEC50 = 5.1 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 897 19 9 6 3.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/ml500340z
CHEMBL3422428 118360 0 None - 1 Mouse 5.1 pEC50 = 5.1 Binding
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 897 19 9 6 3.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/ml500340z
CHEMBL2369972 207998 0 None - 0 Mouse 5.1 pEC50 = 5.1 Binding
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 210418 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207303 0 None - 0 Mouse 5.1 pEC50 = 5.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207309 0 None - 0 Mouse 5.1 pEC50 = 5.1 Binding
Effective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cellsEffective concentration against mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208003 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
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 209963 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 207045 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 209451 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro activation of mouse recombinant Melanocortin-5 receptor.In vitro activation of mouse recombinant Melanocortin-5 receptor.
ChEMBL 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 98064 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276301 98064 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
In vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 5 receptor (MC5R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL2371147 208262 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
ChEMBL 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 10150 0 None - 2 Human 10.6 pIC50 = 10.6 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10150 0 None - 2 Human 10.6 pIC50 = 10.6 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161322 206756 0 None - 2 Human 10.5 pIC50 = 10.5 Binding
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 207452 0 None - 2 Human 10.1 pIC50 = 10.1 Binding
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 83039 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 543 11 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL220018 83039 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 543 11 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
44418438 165446 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL425442 165446 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL1161323 206757 0 None - 2 Human 10.0 pIC50 = 10.0 Binding
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 208408 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 82786 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 500 11 2 3 4.7 O=C(CCc1c[nH]c2ccccc12)NCCCCCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218558 82786 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 500 11 2 3 4.7 O=C(CCc1c[nH]c2ccccc12)NCCCCCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
44418437 82748 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL218361 82748 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 458 8 2 3 3.5 O=C(CCC(=O)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1)NCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.07.015
CHEMBL501592 212360 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 208404 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 141403 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL387169 141403 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
1324 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16154396 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
44285019 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
57514683 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
91898441 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
DB04931 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
1324 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
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 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16154396 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
44285019 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
57514683 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
91898441 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
DB04931 299 23 None -6 4 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL2096742 207452 0 None - 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 208410 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 213837 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 208518 0 None - 2 Human 8.9 pIC50 = 8.9 Binding
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 207410 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 2639 49 None - 3 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2639 49 None - 3 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2639 49 None - 3 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL2371965 208407 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 78057 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 78057 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL203760 207407 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 212185 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 207127 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 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 158763 0 None - 3 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 158763 0 None - 3 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL190551 207312 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210963 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 212735 0 None - 3 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 210415 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 66842 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL187774 66842 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
122184912 122030 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122030 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44397220 166739 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 166739 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL264190 208853 1 None - 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 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
CHEMBL2096759 207454 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 75021 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75021 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL427205 211594 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 14858 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 14858 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
15953833 78549 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 78549 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
137647538 157407 0 None - 3 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 157407 0 None - 3 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137646617 156990 0 None - 3 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 156990 0 None - 3 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL5085972 213220 0 None - 3 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 210069 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 207524 31 None -100 4 Human 6.9 pIC50 = 6.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 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 207524 31 None -100 4 Human 6.9 pIC50 = 6.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 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 207524 31 None -100 4 Human 6.9 pIC50 = 6.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 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 207524 31 None -100 4 Human 6.9 pIC50 = 6.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 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 206755 0 None - 2 Human 7.9 pIC50 = 7.9 Binding
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 163400 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 163400 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
24774521 153712 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398635 153712 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44397652 123104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL361883 123104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
155546131 172948 0 None - 3 Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4531291 172948 0 None - 3 Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
6918276 15420 4 None -12 8 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 15420 4 None -12 8 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
46919520 14954 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 14954 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44431512 145379 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 145379 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL5092761 213603 0 None - 3 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 209992 1 None -29 3 Mouse 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 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 207305 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 213335 0 None - 3 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 94519 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 94519 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
122184578 121902 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600839 121902 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44577515 188410 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 188410 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
49862375 14855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 14855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
54586246 60477 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762008 60477 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL376339 210487 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 100722 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 100722 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 5 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
6918813 130836 2 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 130836 2 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44277696 100722 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 100722 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC5R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
118735103 118285 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118285 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
1324 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16154396 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
44285019 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
57514683 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
91898441 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
DB04931 299 23 None - 4 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
54584301 60471 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
CHEMBL1761872 60471 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
10483153 60472 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 60472 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
54584302 60473 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 60473 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
44397461 125693 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 125693 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL3350396 209723 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 66919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 66919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL539306 66919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-5-receptor (MC5R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
122184575 121899 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 121899 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44408252 140125 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140125 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
127053937 148509 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL3942822 148509 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL2371964 208406 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 147777 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 147777 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
44348144 157268 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)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 157268 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)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 122026 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122026 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5081077 212935 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 190567 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5188894 190567 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
1338 3735 37 None - 4 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3735 37 None - 4 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3735 37 None - 4 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL190203 207310 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210284 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210066 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 161363 0 None -208 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 161363 0 None -208 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 161363 0 None -208 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL1161316 206752 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
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 210060 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 210056 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 164094 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164094 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408189 168302 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168302 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL3349030 209649 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 213493 0 None - 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 155663 0 None - 3 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 155663 0 None - 3 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145964837 163784 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 163784 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL5087859 213339 0 None - 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 118282 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 118282 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3600913 210065 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 213501 0 None - 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 96614 0 None 2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 96614 0 None 2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44408173 75036 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75036 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44408276 75141 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75141 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
132938008 158954 0 None -17 3 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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 158954 0 None -17 3 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@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 166347 71 None -3 4 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 166347 71 None -3 4 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 166347 71 None -3 4 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
168296790 191738 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5206941 191738 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5075712 212613 0 None - 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 212698 0 None - 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 210070 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 212704 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
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 207524 31 None -100 4 Human 7.8 pIC50 = 7.8 Binding
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 96462 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 96462 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
71449047 78056 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 78056 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44577510 188139 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188139 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44408154 140818 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 140818 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL3349030 209649 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 155318 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155318 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
11993702 3523 18 None -19 5 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3523 18 None -19 5 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3523 18 None -19 5 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3523 18 None -19 5 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3523 18 None -19 5 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
10408 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 711 26 None -3 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 213087 0 None - 3 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 213515 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 207311 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207313 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207325 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208382 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 189966 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 189966 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL2371712 208354 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 208413 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 212371 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
16154396 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
16197727 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
44285019 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
57514683 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
91898441 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
DB04931 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
1324 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
16154396 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
44285019 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
57514683 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
91898441 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
DB04931 299 23 None -6 4 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL413573 211317 0 None 1 2 Human 8.7 pIC50 = 8.7 Binding
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 207409 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 211580 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 212382 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 212162 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 212343 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 208409 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 121908 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 121908 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371963 208405 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 164169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217528 164169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408155 140010 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140010 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL439691 212090 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 156722 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 156722 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL1201469 14326 0 None -1 4 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL5076315 212647 0 None - 3 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 95142 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95142 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44417555 96778 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 896 15 9 10 1.2 CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm060768f
CHEMBL268684 96778 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 896 15 9 10 1.2 CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm060768f
CHEMBL2372588 208517 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
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 163680 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4211275 163680 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408388 139780 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 139780 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
24774519 94400 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253788 94400 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL509582 213760 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 75053 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75053 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL409144 210990 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 1468 6 None -3 3 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
16133814 1468 6 None -3 3 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1468 6 None -3 3 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
CHEMBL3600841 210061 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 205185 91 None -61 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -61 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -61 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2247 502 77 None -63 42 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -63 42 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -63 42 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -63 42 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -63 42 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
1323 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
24774438 94401 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253789 94401 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
6918849 122436 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360818 122436 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2371973 208415 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 207514 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 130836 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 130836 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-5 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
16725559 94535 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 94535 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
10077258 14847 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 14847 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL389674 210676 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 1468 6 None -3 3 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16133814 1468 6 None -3 3 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1468 6 None -3 3 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
137659790 158763 0 None - 3 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 158763 0 None - 3 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
122184914 122031 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122031 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
1323 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2639 49 None - 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL228194 207698 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 78322 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 78322 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
1016 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -66 35 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL2221249 207688 0 None -1 3 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None 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 121906 0 None -3 4 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 121906 0 None -3 4 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5091245 213516 0 None - 3 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 153759 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 153759 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600834 210058 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 174357 0 None -19 4 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 174357 0 None -19 4 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL426756 211591 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 159637 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 159637 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
44448631 94614 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 94614 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
49862425 14876 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 14876 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
137631599 155973 0 None - 3 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 155973 0 None - 3 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
2750 202354 69 None -15 12 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202354 69 None -15 12 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
44431511 87624 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL234629 87624 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
155548853 173227 0 None -50 4 Mouse 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 173227 0 None -50 4 Mouse 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL414778 211398 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 210057 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 211312 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 207412 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 190462 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 190462 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
127053935 143641 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 143641 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3752534 210459 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 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 207128 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 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 210548 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 212598 0 None - 3 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 122437 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360819 122437 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
127053935 143641 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 143641 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
71459938 78556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 78556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL189991 207307 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 209071 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210410 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
9938402 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL339053 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
1338 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3735 37 None -144 4 Human 6.5 pIC50 = 6.5 Binding
Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1334 1468 6 None -3 3 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
16133814 1468 6 None -3 3 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1468 6 None -3 3 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL None None None None 10.1021/jm049579s
10210964 66892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL187990 66892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
16157270 210796 15 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 210796 15 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 188227 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 188227 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL376614 210495 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 210796 15 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 210796 15 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 210063 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 209649 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 145979 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3922633 145979 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL227239 207696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 174391 0 None -10 4 Mouse 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 174391 0 None -10 4 Mouse 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
145990599 166291 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 166291 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
118735102 118284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 118284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
2683 102402 24 None -478 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102402 24 None -478 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102402 24 None -478 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
24858481 188510 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 909 12 10 10 2.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL510234 188510 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 909 12 10 10 2.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
145971389 164070 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164070 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
11249545 65857 0 None 61 4 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 65857 0 None 61 4 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11364326 66338 0 None 27 3 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 66338 0 None 27 3 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL5094168 213694 0 None - 3 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 121909 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 121909 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
25444 155099 5 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL404811 155099 5 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
122184636 121907 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 121907 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL375947 210475 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 188352 80 None -50 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188352 80 None -50 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3198 203792 73 None -81 34 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -81 34 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -81 34 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL371610 210413 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL1161320 206754 0 None - 2 Human 8.4 pIC50 = 8.4 Binding
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 168278 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 168278 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
1323 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
92432 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
1323 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2639 49 None - 3 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
163196518 191521 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 191521 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL1161318 206753 0 None - 2 Human 8.3 pIC50 = 8.3 Binding
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 123312 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL362523 123312 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL381739 210535 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 152503 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 152503 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.Radioligand Binding Assay: Radioligand binding and cAMP assays were also conducted using membranes and cells expressing MC5R cloned from other species (mouse MC5R membranes were obtained from Euroscreen; canine, rhesus monkey, cyno monkey and guinea pig MC5 receptors were cloned and expressed from cDNA libraries and transiently transfected as described in Examples 107 and 109. Plasma membranes from the cells were tested in the radioligand assay as in Example 102.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
137655905 158270 0 None - 3 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158270 0 None - 3 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137640703 156543 0 None - 3 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 156543 0 None - 3 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
168272745 189919 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccc(cc2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179534 189919 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccc(cc2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
122184911 122028 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122028 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
1323 2639 49 None - 3 Human 7.4 pIC50 = 7.4 Binding
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 2639 49 None - 3 Human 7.4 pIC50 = 7.4 Binding
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 2639 49 None - 3 Human 7.4 pIC50 = 7.4 Binding
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 60470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 60470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL383250 210555 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 163799 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 163799 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
24857886 154697 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402769 154697 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
68617 203806 60 None -21 26 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 203806 60 None -21 26 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 203806 60 None -21 26 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
145980719 165932 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 165932 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
168274393 189502 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5172938 189502 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11341045 65820 0 None 22 4 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 65820 0 None 22 4 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL3600835 210059 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 212051 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 208412 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 212008 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 207406 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 148788 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3945076 148788 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL190080 207308 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 208378 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 189928 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179637 189928 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5080784 212924 0 None - 3 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 160180 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL411391 160180 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
11341046 66531 0 None 57 4 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 66531 0 None 57 4 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
11237444 126930 0 None 245 3 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 126930 0 None 245 3 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
10304776 78554 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2113041 78554 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
54587278 60478 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 60478 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
44366171 120768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 120768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanocortin 5 receptorBinding affinity against human Melanocortin 5 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL410795 211085 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 212907 0 None - 3 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 208844 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM
ChEMBL 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 207524 31 None -100 4 Human 6.3 pIC50 = 6.3 Binding
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 207524 31 None -100 4 Human 6.3 pIC50 = 6.3 Binding
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 207524 31 None -100 4 Human 6.3 pIC50 = 6.3 Binding
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 207524 31 None -100 4 Human 6.3 pIC50 = 6.3 Binding
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 152503 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 152503 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
24858479 172030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 915 10 10 10 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL449124 172030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 915 10 10 10 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
57854192 152503 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 152503 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3349030 209649 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 210068 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 193788 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL552520 193788 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
137660993 158888 0 None - 3 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 158888 0 None - 3 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145948876 166911 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 166911 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5078687 212798 0 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 212236 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL 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 121905 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 121905 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
122184576 121900 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 121900 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
122184499 121865 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 121865 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600912 210064 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 121904 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 121904 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600736 210055 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 14857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 14857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
145976863 163195 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163195 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44408253 139801 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 139801 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
11477853 66545 0 None 38 3 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 66545 0 None 38 3 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL5094215 213695 0 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 207323 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 210275 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 118281 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 118281 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL411359 211122 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 167678 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL433764 167678 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL11359 76400 0 None -2 4 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL2068237 76400 0 None -2 4 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
10188529 126247 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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 126247 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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 166892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 166892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2310901 207743 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
ChEMBL 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 14846 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 14846 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
137636677 155547 0 None - 3 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 155547 0 None - 3 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44448479 154820 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 154820 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human MC5RBinding affinity to human MC5R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL5090285 213469 0 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 208835 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 191634 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 191634 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
71456245 78551 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 78551 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
1323 2639 49 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2639 49 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2639 49 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL2371969 208411 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 210705 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 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 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
1323 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
1323 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
1323 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
1323 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
1323 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
92432 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2639 49 None - 3 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against hMC5R transfected in HEK293 cellsInhibitory activity against hMC5R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
11375764 66341 0 None 398 3 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 66341 0 None 398 3 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL380638 210514 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 118283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL2371972 208414 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 156510 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 156510 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137653925 158049 0 None - 3 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 158049 0 None - 3 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL2112008 207472 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 213673 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 78323 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 78323 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
137660671 158660 0 None - 3 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 158660 0 None - 3 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44577514 171878 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 171878 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
2726 904 64 None -112 73 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -112 73 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -112 73 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -112 73 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -112 73 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL3349030 209649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 191704 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 191704 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL227833 207697 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC5R expressed in CHO cells
ChEMBL 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 154353 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL400866 154353 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL188459 207303 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 207326 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from mouse melanocortin receptor-5 expressed in 293 HEK cells
ChEMBL 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 122027 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122027 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408286 140124 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 140124 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
9958649 123825 0 None 53 3 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 123825 0 None 53 3 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human Melanocortin 5 receptorInhibition of human Melanocortin 5 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
137641398 157759 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 157759 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11753695 8293 3 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8293 3 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
44397410 123827 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363740 123827 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 5 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
52918026 60469 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 60469 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3349030 209649 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Human Melanocortin 5 receptor expressed in L-cellsBinding affinity for Human Melanocortin 5 receptor expressed in L-cells
ChEMBL 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 159158 0 None - 3 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159158 0 None - 3 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44431513 145264 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391704 145264 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC5R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
44445082 153756 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 153756 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600921 210067 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 213336 0 None - 3 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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 151696 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3968918 151696 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.Radioligand Binding Assay: Assessments of compound binding to human MC5R (hMC5R)) by displacement of an 125I-labeled NDP-MSH receptor ligand peptide were performed essentially as described in the data sheets produced by Perkin Elmer to accompany their frozen hMC5R membranes (Perkin Elmer catalog number RBXMC5M400UA). [125I] NDP-MSH: Radiolabeled in House and Purified by HPLC: Na125I (0.5 mCi, 17.4 Ci/mg) was added to 50 μL sodium phosphate (50 mM, pH 7.4) in an eppendorf tube precoated with IODOGEN. After incubation for 10 mins the phosphate buffer containing the iodine was added to NDP-MSH (10 μl at 1 mg/mL) in a separate eppendorf tube. This was incubated for a further 10 mins. The iodinated NDP-MSH was purified by HPLC on a Zorbax SB 300 column using solvent A: 0.05% TFA and solvent B: 90% acetonitrile 0.045% TFA with a linear gradient, 0-67% B over 60 mins. The 125I NDP-MSH eluted at 52 mins after the unlabeled starting material (48 min) and was counted and stored in the freezer. It was used within 48 hrs, as radioactive decay and ligand decomposition resulted in greatly reduced specific binding observed after 72 hrs. Incubation buffer: 25 mM HEPES-KOH (pH 7.0), 1.5 mM CaCl2, 1 mM MgSO4, 0.1 M NaCl, 1 mM 1,10-phenanthroline, and 1 Complete™ protease inhibitor tablet/100 mL (Roche, catalog number 1873580). Perkin Elmer frozen hMC5 membranes: catalog number RBXMC5M400UA, 0.4 mL/vial; 400 microassays/vial, 0.78 mg/mL protein concentration. Vials of frozen membranes were thawed rapidly immediately before use, diluted with binding buffer and vortexed. Resuspended membranes were kept on ice until they were added to the wells of the plate. Assays were performed in 96 well polypropylene plates. Membranes (0.78 μg 40 μL of a 1:40 dilution in incubation buffer) were added to [125I] NDP-MSH (0.84 nM; 2200 Ci/mmol) and test compounds in a total volume of 140 μL. This was incubated for 1 hr at 37° C. Non-specific binding was determined with 3 mM NDP-MSH. Plates were filtered using a Tomtec cell harvester with GF/A filters (Wallac) (presoaked in 0.6% polyethylenimine) and washed three times with 1.0 mL ice-cold wash buffer (the above incubation buffer without 1,10-phenanthroline and Complete™ protease inhibitor tablet). The filters were dried in a 37° C. oven, placed in a sample bag and 5 mL Betaplatescint (Wallac) was added. Prepared filters were counted in cassettes in a Microbeta Trilux (Wallac) for 1 min.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3600842 210062 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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 190875 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 190875 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
44347838 96182 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL263585 96182 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
71452720 78546 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 78546 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
1337 3357 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3357 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3357 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
176 394 63 None -5 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -5 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -5 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -5 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -5 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
122184577 121901 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 121901 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC5 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1212 1624 45 None -416 66 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -416 66 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -416 66 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -416 66 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -416 66 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44348183 96704 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL268094 96704 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of human melanocortin 5 receptorInhibition of human melanocortin 5 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44396986 67078 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 67078 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL442504 212158 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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 211418 0 None -1 4 Human 9.8 pKi = 9.8 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
CHEMBL414718 211393 0 None -2 4 Human 9.6 pKi = 9.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 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 210978 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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 76553 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 76553 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
1324 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16154396 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16197727 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
44285019 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
57514683 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
91898441 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL441738 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
DB04931 299 23 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL1923667 207334 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 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 207333 0 None -1 3 Human 9.1 pKi = 9.1 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 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 208951 0 None -3 4 Human 9.1 pKi = 9.1 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL 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 208212 0 None -1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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 76554 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684621 76554 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929804 76554 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070246 76554 0 None -10 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
56851058 68716 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57394091 68716 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
91930626 68716 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
CHEMBL1923666 68716 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1823 57 25 20 -0.9 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57646441 76552 0 None -13 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 76552 0 None -13 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57817773 76557 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684623 76557 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929806 76557 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070249 76557 0 None -58 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
9915636 66475 0 None -48 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186083 66475 0 None -48 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44395681 66521 0 None -70 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186289 66521 0 None -70 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
16046215 79664 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
CHEMBL213122 79664 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
16046215 79664 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
CHEMBL213122 79664 0 None -39 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
9915636 66475 0 None -48 4 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL186083 66475 0 None -48 4 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
156010247 176488 0 None -5 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
CHEMBL4633001 176488 0 None -5 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
44434706 89153 0 None -7 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237504 89153 0 None -7 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434860 89597 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238159 89597 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44434632 145764 0 None -1 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392096 145764 0 None -1 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434601 145923 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL392223 145923 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434870 147604 0 None -4 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL393553 147604 0 None -4 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
71454518 78725 0 None -6 4 Human 5.0 pKi = 5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL2113315 78725 0 None -6 4 Human 5.0 pKi = 5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
2817655 203849 5 None - 1 Human 4.0 pKi = 4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 297 4 1 1 5.3 c1ccc2cc(CNCc3cccc4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8129 203849 5 None - 1 Human 4.0 pKi = 4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 297 4 1 1 5.3 c1ccc2cc(CNCc3cccc4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
11191792 66835 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 4.7 CC1C(=O)NCCN1/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL187757 66835 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 4.7 CC1C(=O)NCCN1/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
9958649 123825 0 None 53 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 123825 0 None 53 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL2070373 207432 0 None -14 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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 192761 0 None -26 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL525177 192761 0 None -26 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44577090 178080 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467771 178080 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44577060 187459 0 None -316 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 187459 0 None -316 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434692 88083 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235176 88083 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434841 88259 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 455 11 4 2 4.9 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236022 88259 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 455 11 4 2 4.9 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10137615 89292 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237692 89292 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434754 89791 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 89791 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434862 89803 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238368 89803 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44434600 148058 0 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393918 148058 0 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434763 150799 0 None -17 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL396111 150799 0 None -17 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
6918276 15420 4 None -12 8 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 15420 4 None -12 8 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
168282596 190302 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL5185132 190302 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL2370966 208214 0 None 28 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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 116436 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 116436 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
24848995 117431 0 None -50 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 117431 0 None -50 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44415417 79721 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL213380 79721 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
23635235 165937 0 None -223 5 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 165937 0 None -223 5 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
10232787 139838 0 None -165 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380855 139838 0 None -165 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
24740419 147650 0 None -478 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
CHEMBL393584 147650 0 None -478 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
44397281 126010 0 None -109 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365237 126010 0 None -109 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434694 88159 0 None -5 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235589 88159 0 None -5 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44434611 88172 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL235627 88172 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44435220 88808 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236803 88808 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434701 89057 0 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL237291 89057 0 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
10177247 89070 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237314 89070 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434599 89475 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 333 7 2 2 3.7 NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237957 89475 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 333 7 2 2 3.7 NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434581 166487 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL428903 166487 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
71461662 78691 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2113280 78691 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2070374 207433 0 None -22 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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 178059 0 None -11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467586 178059 0 None -11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44347119 113911 0 None -346 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 113911 0 None -346 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44433294 152497 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL397580 152497 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
23653113 88210 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235798 88210 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434616 88253 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236003 88253 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434570 89335 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237719 89335 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434598 89372 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237743 89372 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168289584 191180 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5198158 191180 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL2370968 208216 0 None -70 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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 16136 0 None -257 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16136 0 None -257 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44323234 167482 0 None -11 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 167482 0 None -11 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11226756 119456 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 119456 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
10211466 168323 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL438432 168323 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44397283 66815 0 None -112 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL187659 66815 0 None -112 3 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44393418 155147 0 None -14 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL405150 155147 0 None -14 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
2852098 203743 13 None 1 3 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8045 203743 13 None 1 3 Human 4.9 pKi = 4.9 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
11272524 66514 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 6 2 2 6.9 CC1CC(C)CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186249 66514 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 6 2 2 6.9 CC1CC(C)CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
57817730 76555 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684622 76555 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929805 76555 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070247 76555 0 None -75 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL438235 212001 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
44347221 16442 0 None -173 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 16442 0 None -173 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
16132144 207524 31 None -100 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
16133793 207524 31 None -100 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
44273719 207524 31 None -100 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
CHEMBL214332 207524 31 None -100 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
44265672 10071 0 None -6 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159699 10071 0 None -6 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44265707 10074 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159701 10074 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434790 89794 0 None 1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238353 89794 0 None 1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434703 145563 0 None -12 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL391944 145563 0 None -12 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434765 161210 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL413982 161210 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
51346771 57903 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL1682208 57903 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL2370553 208115 0 None -10 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
44400935 70503 0 None -104 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
CHEMBL195110 70503 0 None -104 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
44432966 145756 0 None -1659 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL392092 145756 0 None -1659 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44393417 96130 0 None -40 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL263182 96130 0 None -40 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434865 88308 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL236226 88308 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
10200110 89289 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237687 89289 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434828 147578 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393532 147578 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434702 148969 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL394646 148969 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
138106885 166347 71 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 166347 71 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 166347 71 None -3 4 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL2370963 208211 0 None -11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
10408 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
5329 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
9941379 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
CHEMBL2070241 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
DB11653 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 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/jm201489a
16007285 80695 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL215659 80695 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL409049 210988 0 None -141 3 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44434855 89585 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 89585 0 None -4 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44393441 66081 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL185195 66081 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44392514 123336 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362670 123336 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434794 88078 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235147 88078 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434850 88730 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236645 88730 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434656 89578 0 None -6 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 401 10 2 2 5.2 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238136 89578 0 None -6 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 401 10 2 2 5.2 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11284919 65844 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 605 7 2 3 7.3 Cc1ccc(C)c(N2CCN(/C(=N/c3ccc(C(=O)NCCc4ccc(Cl)cc4Cl)cc3)NC3CCCCC3)CC2)c1 10.1021/jm0400496
CHEMBL184385 65844 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 605 7 2 3 7.3 Cc1ccc(C)c(N2CCN(/C(=N/c3ccc(C(=O)NCCc4ccc(Cl)cc4Cl)cc3)NC3CCCCC3)CC2)c1 10.1021/jm0400496
CHEMBL420167 211484 0 None -11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
11341045 65820 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 65820 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
23635107 91113 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
CHEMBL240571 91113 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
23635107 91113 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240571 91113 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44562440 178453 0 None -27 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL471340 178453 0 None -27 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
44392535 63926 0 None -33 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL180937 63926 0 None -33 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434872 88122 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235382 88122 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434758 88252 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL236002 88252 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
9924916 88567 0 None 2 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236447 88567 0 None 2 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434781 89460 0 None -23 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 89460 0 None -23 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
9969456 147072 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393125 147072 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434863 147600 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393552 147600 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
2163781 96915 9 None 1 3 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269653 96915 9 None 1 3 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
168281969 190674 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 190674 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL1201469 14326 0 None -1 4 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL438030 211986 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
44397304 126292 0 None -158 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365465 126292 0 None -158 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
10270570 88591 0 None -4 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236450 88591 0 None -4 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434639 147613 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393557 147613 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168273045 189650 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5175392 189650 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168281969 190674 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 190674 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
11375764 66341 0 None 398 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 66341 0 None 398 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
59149264 76434 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 76434 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 76434 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 76434 0 None -22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL331259 209605 0 None -70 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
44410802 139842 0 None -114 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380858 139842 0 None -114 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
44434661 88071 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL235136 88071 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
44434683 88859 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL236847 88859 0 None -5 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
9946358 151414 0 None 1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCN(CCCc1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396655 151414 0 None 1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCN(CCCc1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434635 168310 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438334 168310 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11364326 66338 0 None 27 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 66338 0 None 27 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL410168 211047 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
CHEMBL427629 211599 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
1334 1468 6 None -3 3 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
16133814 1468 6 None -3 3 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1468 6 None -3 3 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
16038315 138216 0 None -309 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
CHEMBL378046 138216 0 None -309 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
44434685 88727 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236638 88727 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434839 88211 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235802 88211 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434767 89291 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237689 89291 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434682 148060 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393919 148060 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434771 148246 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394073 148246 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
4189 205185 91 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -61 34 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2247 502 77 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL2370533 208113 0 None -10 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
CHEMBL263878 208843 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
156015336 176935 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
CHEMBL4639782 176935 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
44434652 89457 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237912 89457 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434707 149003 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL394667 149003 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
10077773 86825 4 None -1122 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233135 86825 4 None -1122 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434769 89295 0 None -13 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237698 89295 0 None -13 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434857 153880 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398980 153880 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168286369 191106 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5197030 191106 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168283984 190642 0 None -3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190172 190642 0 None -3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
11785639 126928 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.3 NC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
CHEMBL366036 126928 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 5.3 NC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
44400812 70941 0 None -457 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 667 12 3 5 6.3 O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195734 70941 0 None -457 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 667 12 3 5 6.3 O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11156852 65339 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL183434 65339 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
11156852 65339 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
CHEMBL183434 65339 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
44434592 89071 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237315 89071 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434753 89290 0 None -9 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 699 12 3 4 9.1 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
CHEMBL237688 89290 0 None -9 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 699 12 3 4 9.1 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
10159196 89294 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237694 89294 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10269187 89671 0 None -4 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.5 NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL238180 89671 0 None -4 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.5 NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434868 149007 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL394669 149007 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL407809 210928 0 None -851 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL433645 211885 0 None -6 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
CHEMBL428326 211680 0 None -47 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
24873537 145516 0 None -20 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 145516 0 None -20 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
11181804 127972 0 None -21 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 127972 0 None -21 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44434562 88256 0 None -301 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236014 88256 0 None -301 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
44347378 113923 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333262 113923 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434843 88258 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 88258 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434657 89789 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 89789 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
1016 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -66 35 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL2221249 207688 0 None -1 3 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None 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
168271899 189997 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5180727 189997 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44433264 88907 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236940 88907 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44347379 113924 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333263 113924 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44265496 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
9968756 89065 0 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237299 89065 0 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
10292084 147851 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL393755 147851 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434614 151040 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396341 151040 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265496 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL267020 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL266417 208928 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
44322868 105515 0 None -4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 105515 0 None -4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11341046 66531 0 None 57 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 66531 0 None 57 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
44394079 126231 0 None -9 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL365278 126231 0 None -9 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
71461657 78614 0 None 4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113144 78614 0 None 4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44434845 147358 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393350 147358 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
2750 202354 69 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202354 69 None -15 12 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL439128 212067 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
10033237 68714 0 None -158 3 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
CHEMBL1923662 68714 0 None -158 3 Human 7.6 pKi = 7.6 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
CHEMBL2070254 207431 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11296600 122415 0 None -41 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 122415 0 None -41 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44347106 114549 0 None -46 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL334309 114549 0 None -46 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44265496 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 96589 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
10132207 88209 0 None -7 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 343 5 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235797 88209 0 None -7 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 343 5 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434843 88258 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 88258 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL268851 209014 0 None -33 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
168279695 190531 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 190531 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168285313 190797 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 190797 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
6918814 126523 1 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL365597 126523 1 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
58777892 78619 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
CHEMBL2113149 78619 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
44434799 88161 0 None 1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235592 88161 0 None 1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434653 145270 0 None -36 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391706 145270 0 None -36 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265347 96506 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL266305 96506 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
11192466 65741 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 577 7 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm0400496
CHEMBL183842 65741 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 577 7 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm0400496
9946241 88988 0 None -7 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237079 88988 0 None -7 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434687 158933 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410179 158933 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
70688853 76556 0 None -9 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070248 76556 0 None -9 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57817763 76559 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 76559 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 76559 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 76559 0 None -38 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
59149255 76560 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 76560 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 76560 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 76560 0 None -13 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
56851059 68717 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
57390568 68717 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
91930628 68717 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
CHEMBL1923668 68717 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1784 57 24 20 -1.4 C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C 10.1021/jm201226w
168279695 190531 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 190531 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44400864 123793 0 None -177 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363576 123793 0 None -177 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11410616 64928 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 579 7 2 5 5.7 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ncccn3)CC2)cc1 10.1021/jm0400496
CHEMBL182844 64928 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 579 7 2 5 5.7 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(c3ncccn3)CC2)cc1 10.1021/jm0400496
44322869 105667 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 105667 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44434603 89469 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237935 89469 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434686 146055 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL392316 146055 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
23635237 91008 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
CHEMBL240364 91008 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
23635237 91008 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL240364 91008 0 None -53 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
44434688 88729 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236640 88729 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434690 88862 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 88862 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434587 88994 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237094 88994 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434849 146311 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL392521 146311 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
168295173 191703 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 191703 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44562414 176233 0 None -13 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL460942 176233 0 None -13 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL2370965 208213 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
44434597 89169 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237530 89169 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44577093 178060 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467587 178060 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
23635235 165937 0 None -223 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
CHEMBL427860 165937 0 None -223 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
23635236 91155 0 None -60 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240780 91155 0 None -60 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434584 151398 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL396638 151398 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
10180932 88963 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237051 88963 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434658 89790 0 None -3 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 89790 0 None -3 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
10225762 145272 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL391707 145272 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
2683 102402 24 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102402 24 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102402 24 None -478 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
44400934 70254 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194987 70254 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44400813 70727 0 None -120 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195308 70727 0 None -120 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
11785893 66670 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 530 6 2 3 6.0 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)O1 10.1021/jm0400496
CHEMBL187022 66670 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 530 6 2 3 6.0 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)O1 10.1021/jm0400496
10108894 89293 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
CHEMBL237693 89293 0 None -5 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
44434621 145760 0 None -11 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL392094 145760 0 None -11 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
11477853 66545 0 None 38 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 66545 0 None 38 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
44434568 88732 0 None -81 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236650 88732 0 None -81 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
23635236 91155 0 None -60 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
CHEMBL240780 91155 0 None -60 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5RDisplacement of [125I]NDP-MSH from human MC5R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
11443753 66497 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 516 10 2 2 7.0 CCCN(CCC)/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL186189 66497 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 516 10 2 2 7.0 CCCN(CCC)/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
44434696 148654 0 None -36 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394394 148654 0 None -36 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265487 96921 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269689 96921 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
10025669 96929 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269776 96929 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
25444 155099 5 None - 1 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL404811 155099 5 None - 1 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 1229 14 17 29 -6.5 C[C@H]1[C@H]2[C@@H](O[C@]13CC[C@@H](C)CO3)[C@@H](O)[C@H]1[C@@H]3CC[C@H]4C[C@@H](O[C@@H]5O[C@H](CO)[C@H](O[C@@H]6O[C@H](CO)C(O)[C@H](O[C@@H]7OC[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O[C@@H]6O[C@H](CO)[C@H](O)[C@H](O[C@@H]7O[C@H](CO)[C@@H](O)[C@H](O)[C@H]7O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)C[C@]4(C)[C@H]3CC[C@@]12C nan
CHEMBL412523 211243 0 None -125 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
8447 188352 80 None -50 13 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188352 80 None -50 13 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
44265711 205251 0 None -2 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 205251 0 None -2 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434847 88515 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236442 88515 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434864 89804 0 None -13 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238369 89804 0 None -13 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
3198 203792 73 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -81 34 Human 4.4 pKi = 4.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44433439 89480 0 None -44 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL237976 89480 0 None -44 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human MC5 receptorBinding affinity at human MC5 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44434684 146054 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392315 146054 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265312 203944 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 286 4 2 1 4.6 c1ccc2c(CNCc3c[nH]c4ccccc34)cccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8208 203944 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 286 4 2 1 4.6 c1ccc2c(CNCc3c[nH]c4ccccc34)cccc2c1 10.1016/s0960-894x(02)00088-4
51346770 57904 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
CHEMBL1682209 57904 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC5 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
44577094 178061 0 None -117 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467588 178061 0 None -117 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434766 154164 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154164 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44320339 204393 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL85918 204393 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
10025669 96929 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL269776 96929 0 None -57 4 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 5 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL385465 210594 0 None -44 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
CHEMBL2070244 207430 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
59149266 76558 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693081 76558 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929807 76558 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070250 76558 0 None -234 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44347331 16136 0 None -257 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16136 0 None -257 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44577063 187507 0 None -74 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL498150 187507 0 None -74 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
71458055 78603 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
CHEMBL2113133 78603 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
44434689 88731 0 None -33 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236649 88731 0 None -33 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434861 89802 0 None -9 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238367 89802 0 None -9 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168285313 190797 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 190797 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44265374 204752 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8825 204752 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL415661 211440 0 None -295 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
10283036 139700 0 None -72 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380540 139700 0 None -72 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
44265749 205482 0 None -4 3 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 205482 0 None -4 3 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434778 89299 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89299 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
10178845 89470 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237937 89470 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434762 152464 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 152464 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44265309 203939 1 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8201 203939 1 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
68617 203806 60 None -21 26 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 203806 60 None -21 26 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 203806 60 None -21 26 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
11433304 66321 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 591 8 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0400496
CHEMBL185398 66321 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 591 8 2 3 6.9 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0400496
44434704 88728 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236639 88728 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434780 147628 0 None -9 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 525 8 2 2 7.3 NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393568 147628 0 None -9 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 525 8 2 2 7.3 NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1 10.1016/j.bmc.2007.06.003
44265351 204041 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 8 2 3 4.7 N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8287 204041 0 None 1 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 426 8 2 3 4.7 N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
56851057 68715 0 None -190 3 Human 7.3 pKi = 7.3 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1069 34 13 10 1.3 C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1021/jm201226w
CHEMBL1923664 68715 0 None -190 3 Human 7.3 pKi = 7.3 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL 1069 34 13 10 1.3 C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1021/jm201226w
44434662 88072 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235137 88072 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434636 88856 0 None 1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236841 88856 0 None 1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434647 89146 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
CHEMBL237483 89146 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
44397028 123500 0 None -61 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
CHEMBL363019 123500 0 None -61 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
44434690 88862 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 88862 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265472 204622 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8742 204622 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL441760 212138 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC(C)(C)[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44397030 67017 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL188651 67017 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44347105 112834 0 None -43 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL331728 112834 0 None -43 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434854 89584 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 89584 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434855 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44347082 163345 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL420727 163345 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347081 168051 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL436169 168051 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434772 88155 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88155 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434690 88862 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 88862 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10109225 154122 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL399624 154122 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434867 88081 0 None -22 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL235162 88081 0 None -22 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434714 147848 0 None -10 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393753 147848 0 None -10 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL2070242 207429 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11237444 126930 0 None 245 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 126930 0 None 245 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
11249545 65857 0 None 61 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 65857 0 None 61 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11752660 65831 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 2 3 5.1 CN1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
CHEMBL184323 65831 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 2 3 5.1 CN1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC1 10.1021/jm0400496
16007264 79295 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL211564 79295 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
16007264 79295 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
CHEMBL211564 79295 0 None -26 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
44347110 113597 0 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL332762 113597 0 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
1338 3735 37 None -144 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
9938402 3735 37 None -144 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL339053 3735 37 None -144 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
44434713 89152 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 89152 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434855 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44265713 205094 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 364 6 3 4 1.9 O=C(NCCc1c[nH]cn1)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9048 205094 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 364 6 3 4 1.9 O=C(NCCc1c[nH]cn1)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434663 88073 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235138 88073 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
24740655 88643 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
CHEMBL236521 88643 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
24740655 88643 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL236521 88643 0 None -891 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
44434760 88075 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235140 88075 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434764 88118 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235358 88118 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10157774 88857 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236842 88857 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434859 89589 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
CHEMBL238158 89589 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
168295173 191703 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 191703 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC5R expressed in CHO cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44456219 154887 0 None -112 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL403806 154887 0 None -112 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44347219 16388 0 None -1071 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 16388 0 None -1071 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
25211670 173678 0 None -56 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454916 173678 0 None -56 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
44562460 188666 0 None -165 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL511826 188666 0 None -165 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
6918850 124889 1 None -154 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
CHEMBL364560 124889 1 None -154 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
44434690 88862 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 88862 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434654 89576 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238134 89576 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434665 147404 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393383 147404 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434772 88155 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88155 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434778 89299 0 None -10 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89299 0 None -10 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434595 148328 0 None -7 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 419 9 2 3 5.6 CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL394149 148328 0 None -7 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 419 9 2 3 5.6 CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
6918844 168046 1 None -173 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
CHEMBL436122 168046 1 None -173 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
11179871 123692 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 4.5 O=C1CN(/C(=N\C2CCCCC2)Nc2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)CCN1 10.1021/jm0400496
CHEMBL363440 123692 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 515 6 3 3 4.5 O=C1CN(/C(=N\C2CCCCC2)Nc2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)CCN1 10.1021/jm0400496
44434855 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 89585 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44265591 171467 0 None -1 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL447178 171467 0 None -1 3 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44434634 88855 0 None -31 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236840 88855 0 None -31 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
44323020 168419 0 None -741 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 168419 0 None -741 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL1923663 207332 0 None -31 3 Human 7.2 pKi = 7.2 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None CC(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm201226w
10134057 88215 0 None -32 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235815 88215 0 None -32 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11786860 65987 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185035 65987 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44432964 87011 0 None -1513 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233372 87011 0 None -1513 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL2370154 208046 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 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
11215758 65733 0 None -125 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptorBinding affinity for human melanocortin 5 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL183799 65733 0 None -125 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptorBinding affinity for human melanocortin 5 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
24180592 96552 0 None -177 6 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 96552 0 None -177 6 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44265708 166255 0 None -2 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL428480 166255 0 None -2 2 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL11359 76400 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
CHEMBL2068237 76400 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
44434821 89583 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238149 89583 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL427666 211606 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O 10.1021/jm0501432
44434848 88526 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL236443 88526 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44347840 161363 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
91932630 161363 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL415333 161363 0 None -208 3 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 5 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44347220 167865 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 167865 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434766 154164 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154164 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44322795 205189 0 None -114 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 205189 0 None -114 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44265715 10075 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159702 10075 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434856 153846 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398777 153846 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44577091 178081 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467772 178081 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434778 89299 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89299 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434651 89456 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237911 89456 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434698 170448 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL445669 170448 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44400863 68807 0 None -151 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192464 68807 0 None -151 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434855 89585 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 89585 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434785 148247 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394074 148247 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
11295934 66626 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 558 8 3 2 7.1 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\Cc2cc(F)cc(F)c2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186792 66626 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 558 8 3 2 7.1 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\Cc2cc(F)cc(F)c2)NC2CCCCC2)cc1 10.1021/jm0400496
10325955 164708 0 None -6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 164708 0 None -6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 5 receptor (MC5R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
71452732 78609 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113139 78609 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 5 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44347330 167489 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432407 167489 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
70693083 76561 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929813 76561 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070253 76561 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
24740653 88150 0 None -190 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL235556 88150 0 None -190 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
2726 904 64 None -112 73 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -112 73 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -112 73 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -112 73 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -112 73 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL407213 210891 0 None -169 3 Human 6.1 pKi = 6.1 Binding
Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 5 (hMC5R) (concentration of the peptide at 50% specific binding)
ChEMBL 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
11180881 66472 0 None -47 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
CHEMBL186074 66472 0 None -47 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
44434695 88982 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237070 88982 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434768 154165 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL399811 154165 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44400660 70371 0 None -301 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195071 70371 0 None -301 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeledBinding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44396002 124241 0 None -17 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
CHEMBL364215 124241 0 None -17 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
10158674 147370 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393359 147370 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265589 204587 0 None -2 2 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
CHEMBL8720 204587 0 None -2 2 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 499 12 7 4 2.3 N=C(N)NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(02)00089-6
44265479 204359 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 268 2 2 2 1.9 N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(02)00088-4
CHEMBL8561 204359 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 268 2 2 2 1.9 N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(02)00088-4
44434713 89152 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 89152 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
16172929 211244 17 None -87 4 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
CHEMBL412536 211244 17 None -87 4 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
44434754 89791 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 89791 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
11365127 123557 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 569 7 2 3 6.6 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCC(N3CCCC3)CC2)cc1 10.1021/jm0400496
CHEMBL363290 123557 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 569 7 2 3 6.6 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCC(N3CCCC3)CC2)cc1 10.1021/jm0400496
44434782 89582 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238144 89582 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434772 88155 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88155 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434637 88968 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237052 88968 0 None 1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL409636 211016 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.
ChEMBL 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
44456222 97463 0 None -676 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 97463 0 None -676 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC5RBinding affinity to MC5R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44434666 88117 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235356 88117 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
44434650 89455 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237910 89455 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434648 147615 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393558 147615 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44393421 122574 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL361052 122574 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434797 88160 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235590 88160 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434691 88981 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL237069 88981 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434770 88119 0 None -46 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235359 88119 0 None -46 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44265473 204623 1 None -9 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 200 4 2 2 1.9 NCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8743 204623 1 None -9 2 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 5 receptor by using radioligand binding assay
ChEMBL 200 4 2 2 1.9 NCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
44434690 89461 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237920 89461 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
24180646 147638 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 147638 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC5RBinding affinity at human MC5R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
24180646 147638 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 147638 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
44434633 88726 0 None -35 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236630 88726 0 None -35 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434699 89056 0 None -26 3 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 531 10 2 3 7.7 CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237290 89056 0 None -26 3 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 531 10 2 3 7.7 CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
24741624 137839 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL377231 137839 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC5R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
24741624 137839 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL377231 137839 0 None -6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NDPMSH from human MC5R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC5R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
1338 3735 37 None -144 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
9938402 3735 37 None -144 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL339053 3735 37 None -144 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
44265639 10069 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159697 10069 0 None -6 4 Human 5.1 pKi = 5.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
44434884 88169 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235617 88169 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434690 88862 0 None -8 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 88862 0 None -8 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434655 89577 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238135 89577 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10260053 167629 0 None -6 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 167629 0 None -6 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
44432932 87312 0 None -263 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233758 87312 0 None -263 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 5 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434700 148965 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 637 12 3 4 9.0 CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL394645 148965 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 637 12 3 4 9.0 CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434762 152464 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 152464 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
10155513 150997 0 None -9 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396303 150997 0 None -9 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
176 394 63 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -5 31 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
1212 1624 45 None -416 66 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -416 66 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -416 66 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -416 66 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -416 66 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
1324 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
16154396 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
16197727 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
44285019 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
57514683 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
91898441 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
CHEMBL441738 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
DB04931 299 23 None -6 4 Human 8.0 pKi = 8 Binding
Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis
ChEMBL None None None None 10.1021/jm201226w
11318528 65908 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 7 2 2 7.1 CN(/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1)C1CCCCC1 10.1021/jm0400496
CHEMBL184612 65908 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cellsInhibition of [125I]NDP-MSH binding to human Melanocortin 5 receptor expressed in HEK293 cells
ChEMBL 528 7 2 2 7.1 CN(/C(=N/c1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1)C1CCCCC1 10.1021/jm0400496
44410803 139629 0 None -87 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380365 139629 0 None -87 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44434880 88168 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235616 88168 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434709 89331 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237714 89331 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434854 89584 0 None -1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 89584 0 None -1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434787 148248 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394075 148248 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434605 148970 0 None -13 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
CHEMBL394647 148970 0 None -13 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
10304463 76406 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL206840 76406 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
44397198 66417 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL185862 66417 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
10291370 145421 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391823 145421 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434772 88155 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88155 0 None -6 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44393450 123124 0 None -2 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362010 123124 0 None -2 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44562287 173666 0 None -102 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454900 173666 0 None -102 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
6918857 138167 1 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL377961 138167 1 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC5R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
44434693 166782 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL429451 166782 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44265719 205391 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL9219 205391 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 5 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1ccc2ccccc2c1)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44434697 148149 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL393994 148149 0 None -4 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434759 88074 0 None -23 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235139 88074 0 None -23 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
25058412 188840 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL513404 188840 0 None -120 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to MC5 receptorBinding affinity to MC5 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434851 89465 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237930 89465 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434761 88723 0 None -14 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236626 88723 0 None -14 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC5 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10257541 125808 0 None -602 4 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL365039 125808 0 None -602 4 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Melanocortin 5 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 5 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
46877881 200123 0 None -5 3 Human 6.0 pKi = 6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 200123 0 None -5 3 Human 6.0 pKi = 6 Binding
Binding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cellsBinding affinity for human melanocortin 5 receptor (hMC5R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11296732 143269 0 None -22 3 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL390130 143269 0 None -22 3 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 5 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
23661656 168467 0 None -181 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 168467 0 None -181 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]NDP-MSH from MC5R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC5R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
11296732 143269 0 None -22 3 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL390130 143269 0 None -22 3 Human 6.0 pKi = 6 Binding
Displacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC5 receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
1329 311 0 None -5011 3 Mouse 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
1320 363 0 None -19 3 Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
16162729 363 0 None -19 3 Human 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1328 1904 0 None -10 4 Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9832440
1325 3530 12 None -15 7 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
6440621 3530 12 None -15 7 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
9898183 3530 12 None -15 7 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
CHEMBL3422426 3530 12 None -15 7 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
None 214548 0 125I-NDP-MSH -8511 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
None 214548 0 125I-[Nle4,D-Phe7]Alpha-MSH -8511 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
None 214549 0 125I-NDP-MSH -93 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 961 29 13 12 -1.5 CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N None
None 214549 0 125I-[Nle4,D-Phe7]Alpha-MSH -93 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 961 29 13 12 -1.5 CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N None
3198 203792 73 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203792 73 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203792 73 None -81 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1016 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3678 75 None -66 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
4189 205185 91 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205185 91 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205185 91 None -61 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
138106885 166347 71 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
36314 166347 71 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
CHEMBL428647 166347 71 None -3 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
176 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
1212 1624 45 None -416 66 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 None -416 66 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 None -416 66 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 None -416 66 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 None -416 66 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2726 904 64 None -112 73 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 None -112 73 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 None -112 73 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 None -112 73 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 None -112 73 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
68617 203806 60 None -21 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203806 60 None -21 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203806 60 None -21 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2247 502 77 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
11993702 3523 18 None -19 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
5416 3523 18 None -19 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
9272 3523 18 None -19 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
CHEMBL3301624 3523 18 None -19 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
DB11700 3523 18 None -19 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
10408 711 26 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
5329 711 26 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379 711 26 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
CHEMBL2070241 711 26 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
DB11653 711 26 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
10408 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 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 22335602
5329 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 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 22335602
9941379 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 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 22335602
CHEMBL2070241 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 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 22335602
DB11653 711 26 None -3 4 Human 7.8 pKi = 7.8 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>5</sub> receptor.
Guide to Pharmacology 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 22335602
11993702 3523 18 None -19 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
5416 3523 18 None -19 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
9272 3523 18 None -19 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
CHEMBL3301624 3523 18 None -19 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
DB11700 3523 18 None -19 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
134611880 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
16132265 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
3633 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
4931 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
CHEMBL1201610 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
DB01285 275 0 None -2187 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675