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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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H don H acc LogP Smiles DOI
1324 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 203686 0 MC5R MC5 receptor 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
44366081 9985 0 MC5R MC5 receptor 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 9985 0 MC5R MC5 receptor 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
118722937 115495 0 MC5R MC5 receptor 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 115495 0 MC5R MC5 receptor 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 115499 0 MC5R MC5 receptor 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 115499 0 MC5R MC5 receptor 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 115492 0 MC5R MC5 receptor 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 115492 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
1323 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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
118722944 115502 0 MC5R MC5 receptor 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 115502 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
1324 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 202035 0 MC5R MC5 receptor 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
CHEMBL414965 206678 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 115490 0 MC5R MC5 receptor 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 115490 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
1324 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
CHEMBL405087 206054 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 206137 0 MC5R MC5 receptor 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 206567 0 MC5R MC5 receptor 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 135660 0 MC5R MC5 receptor 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 135660 0 MC5R MC5 receptor 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
CHEMBL2096742 202730 0 MC5R MC5 receptor 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
CHEMBL410404 206332 0 MC5R MC5 receptor 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
CHEMBL442504 207427 0 MC5R MC5 receptor 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
118722926 115487 0 MC5R MC5 receptor 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 115487 0 MC5R MC5 receptor 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 115491 0 MC5R MC5 receptor 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 115491 0 MC5R MC5 receptor 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 115496 0 MC5R MC5 receptor 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 115496 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 135660 0 MC5R MC5 receptor 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 135660 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 206396 0 MC5R MC5 receptor 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 115500 0 MC5R MC5 receptor 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 115500 0 MC5R MC5 receptor 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 115501 0 MC5R MC5 receptor 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 115501 0 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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
1323 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 80940 0 MC5R MC5 receptor 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 80940 0 MC5R MC5 receptor 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
44327392 141062 0 MC5R MC5 receptor 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 141062 0 MC5R MC5 receptor 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
CHEMBL2371851 203662 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 206069 0 MC5R MC5 receptor 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 115488 0 MC5R MC5 receptor 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 115488 0 MC5R MC5 receptor 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 123203 0 MC5R MC5 receptor 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 123203 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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
CHEMBL1161323 202036 0 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 206248 0 MC5R MC5 receptor 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 114776 0 MC5R MC5 receptor 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 114776 0 MC5R MC5 receptor 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 203689 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 123203 0 MC5R MC5 receptor 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 123203 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 203691 0 MC5R MC5 receptor 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 207565 0 MC5R MC5 receptor 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 158427 0 MC5R MC5 receptor 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 158427 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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
45487403 191026 0 MC5R MC5 receptor 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 191026 0 MC5R MC5 receptor 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 115494 0 MC5R MC5 receptor 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 115494 0 MC5R MC5 receptor 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 203682 0 MC5R MC5 receptor 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
CHEMBL2369959 203263 0 MC5R MC5 receptor 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
CHEMBL267794 204248 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 204495 0 MC5R MC5 receptor 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 204198 0 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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
CHEMBL2371967 203687 0 MC5R MC5 receptor 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 155846 0 MC5R MC5 receptor 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 155846 0 MC5R MC5 receptor 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 111012 0 MC5R MC5 receptor 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 111012 0 MC5R MC5 receptor 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
CHEMBL2369967 203271 0 MC5R MC5 receptor 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
CHEMBL386081 205888 0 MC5R MC5 receptor 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 207028 0 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 206351 0 MC5R MC5 receptor 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 203150 0 MC5R MC5 receptor 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 206394 0 MC5R MC5 receptor 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 96640 0 MC5R MC5 receptor 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 96640 0 MC5R MC5 receptor 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 96640 0 MC5R MC5 receptor 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
1323 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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
10078903 67446 0 MC5R MC5 receptor 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 67446 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 204142 0 MC5R MC5 receptor 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 111015 0 MC5R MC5 receptor 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 111015 0 MC5R MC5 receptor 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 206984 0 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 121780 0 MC5R MC5 receptor 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 121780 0 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 111011 0 MC5R MC5 receptor 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 111011 0 MC5R MC5 receptor 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 70543 0 MC5R MC5 receptor 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 70543 0 MC5R MC5 receptor 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 155171 0 MC5R MC5 receptor 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 155171 0 MC5R MC5 receptor 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
CHEMBL2369964 203268 0 MC5R MC5 receptor 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
CHEMBL2371968 203688 0 MC5R MC5 receptor 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 203690 0 MC5R MC5 receptor 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
137653739 157871 0 MC5R MC5 receptor Human 9.0 pEC50 = 9 ADMET
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 1632 51 23 21 -3.6 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)CN[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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.7b01295
CHEMBL4093140 157871 0 MC5R MC5 receptor Human 9.0 pEC50 = 9 ADMET
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 1632 51 23 21 -3.6 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)CN[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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.7b01295
90643808 111016 0 MC5R MC5 receptor 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 111016 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
44322868 105290 0 MC5R MC5 receptor 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 105290 0 MC5R MC5 receptor 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
1324 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 121659 0 MC5R MC5 receptor 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 121659 0 MC5R MC5 receptor 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 111013 0 MC5R MC5 receptor 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 111013 0 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202730 0 MC5R MC5 receptor 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 206972 0 MC5R MC5 receptor 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 173337 0 MC5R MC5 receptor 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 173337 0 MC5R MC5 receptor 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 202359 0 MC5R MC5 receptor 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 207502 0 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 2527 44 MC5R MC5 receptor 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 203683 0 MC5R MC5 receptor 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 207548 0 MC5R MC5 receptor 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 204748 0 MC5R MC5 receptor 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 173492 0 MC5R MC5 receptor 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 173492 0 MC5R MC5 receptor 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
118722939 115497 0 MC5R MC5 receptor 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 115497 0 MC5R MC5 receptor 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 203492 0 MC5R MC5 receptor 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 115498 0 MC5R MC5 receptor 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 115498 0 MC5R MC5 receptor 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 205082 0 MC5R MC5 receptor 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
CHEMBL503229 207587 0 MC5R MC5 receptor Human 8.7 pEC50 = 8.7 ADMET
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 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/acs.jmedchem.7b01295
145976863 162933 0 MC5R MC5 receptor 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 162933 0 MC5R MC5 receptor 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 207587 0 MC5R MC5 receptor 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 207431 0 MC5R MC5 receptor 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 115493 0 MC5R MC5 receptor 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 115493 0 MC5R MC5 receptor 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
CHEMBL2369963 203267 0 MC5R MC5 receptor 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
1324 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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
CHEMBL1161318 202032 0 MC5R MC5 receptor 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
11787684 69697 0 MC5R MC5 receptor 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 69697 0 MC5R MC5 receptor 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 205729 0 MC5R MC5 receptor 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
CHEMBL347364 205227 0 MC5R MC5 receptor 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 202603 0 MC5R MC5 receptor 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
10483153 60265 0 MC5R MC5 receptor 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 60265 0 MC5R MC5 receptor 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 14688 0 MC5R MC5 receptor 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 14688 0 MC5R MC5 receptor 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 155771 0 MC5R MC5 receptor 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 155771 0 MC5R MC5 receptor 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 11994 0 MC5R MC5 receptor 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 11994 0 MC5R MC5 receptor 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 11994 0 MC5R MC5 receptor 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
CHEMBL365794 205555 0 MC5R MC5 receptor 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
CHEMBL407213 206161 0 MC5R MC5 receptor 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 173667 0 MC5R MC5 receptor 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 173667 0 MC5R MC5 receptor 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
11038873 171041 0 MC5R MC5 receptor 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 171041 0 MC5R MC5 receptor 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
11017471 31509 0 MC5R MC5 receptor 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 31509 0 MC5R MC5 receptor 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 166629 0 MC5R MC5 receptor 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 166629 0 MC5R MC5 receptor 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 207543 1 MC5R MC5 receptor 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 207543 1 MC5R MC5 receptor 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
45487296 190916 0 MC5R MC5 receptor 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 190916 0 MC5R MC5 receptor 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 190609 0 MC5R MC5 receptor 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 190609 0 MC5R MC5 receptor 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 205328 0 MC5R MC5 receptor 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 155670 0 MC5R MC5 receptor 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 155670 0 MC5R MC5 receptor 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 204123 1 MC5R MC5 receptor 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 174449 0 MC5R MC5 receptor 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 174449 0 MC5R MC5 receptor 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 204738 0 MC5R MC5 receptor 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 203040 0 MC5R MC5 receptor 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 93376 0 MC5R MC5 receptor 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 93376 0 MC5R MC5 receptor 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
10260053 167369 0 MC5R MC5 receptor 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 167369 0 MC5R MC5 receptor 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
44441685 93459 0 MC5R MC5 receptor 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 93459 0 MC5R MC5 receptor 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 204739 0 MC5R MC5 receptor 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 204014 0 MC5R MC5 receptor 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 201982 0 MC5R MC5 receptor 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 191027 0 MC5R MC5 receptor 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 191027 0 MC5R MC5 receptor 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
CHEMBL347216 205226 0 MC5R MC5 receptor 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 202586 0 MC5R MC5 receptor 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
44408388 139527 0 MC5R MC5 receptor 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 139527 0 MC5R MC5 receptor 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 172851 0 MC5R MC5 receptor 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 172851 0 MC5R MC5 receptor 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
CHEMBL275303 204336 0 MC5R MC5 receptor 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
44448479 154564 0 MC5R MC5 receptor 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 154564 0 MC5R MC5 receptor 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 155499 0 MC5R MC5 receptor 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 155499 0 MC5R MC5 receptor 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 155499 0 MC5R MC5 receptor 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 203033 0 MC5R MC5 receptor 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
CHEMBL432027 207143 0 MC5R MC5 receptor 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
11061068 30886 0 MC5R MC5 receptor 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 30886 0 MC5R MC5 receptor 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 190560 0 MC5R MC5 receptor 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 190560 0 MC5R MC5 receptor 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 174925 0 MC5R MC5 receptor 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 174925 0 MC5R MC5 receptor 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 174946 0 MC5R MC5 receptor 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 174946 0 MC5R MC5 receptor 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
137653704 157809 0 MC5R MC5 receptor 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 157809 0 MC5R MC5 receptor 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
46877881 195402 0 MC5R MC5 receptor 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 195402 0 MC5R MC5 receptor 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
155550338 173463 0 MC5R MC5 receptor 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 173463 0 MC5R MC5 receptor 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 203116 0 MC5R MC5 receptor 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 155945 0 MC5R MC5 receptor 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 155945 0 MC5R MC5 receptor 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
CHEMBL94391 208001 0 MC5R MC5 receptor 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
145966490 163538 0 MC5R MC5 receptor 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 163538 0 MC5R MC5 receptor 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 163124 0 MC5R MC5 receptor 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 163124 0 MC5R MC5 receptor 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
155538472 172406 0 MC5R MC5 receptor 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 172406 0 MC5R MC5 receptor 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 206869 0 MC5R MC5 receptor 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 60266 0 MC5R MC5 receptor 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 60266 0 MC5R MC5 receptor 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 11993 0 MC5R MC5 receptor 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 11993 0 MC5R MC5 receptor 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 11993 0 MC5R MC5 receptor 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 76571 0 MC5R MC5 receptor 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 76571 0 MC5R MC5 receptor 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 76571 0 MC5R MC5 receptor 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 203007 0 MC5R MC5 receptor 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 207892 0 MC5R MC5 receptor 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
CHEMBL327479 204808 0 MC5R MC5 receptor 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
CHEMBL1090484 7693 0 MC5R MC5 receptor 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 196668 0 MC5R MC5 receptor 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 196668 0 MC5R MC5 receptor 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 121781 0 MC5R MC5 receptor 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 121781 0 MC5R MC5 receptor 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
CHEMBL433522 207153 0 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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
CHEMBL190551 202590 0 MC5R MC5 receptor 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 205230 0 MC5R MC5 receptor 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 167222 0 MC5R MC5 receptor 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 167222 0 MC5R MC5 receptor 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
CHEMBL228194 202976 0 MC5R MC5 receptor 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
CHEMBL1093858 8205 0 MC5R MC5 receptor 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 205341 0 MC5R MC5 receptor 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 121652 0 MC5R MC5 receptor 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 121652 0 MC5R MC5 receptor 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 58275 0 MC5R MC5 receptor 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 58275 0 MC5R MC5 receptor 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 58275 0 MC5R MC5 receptor 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 58275 0 MC5R MC5 receptor 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
137651074 156652 0 MC5R MC5 receptor Human 7.8 pEC50 = 7.8 ADMET
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 1511 43 21 17 -2.2 CC(C)C[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](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/acs.jmedchem.7b01295
CHEMBL4079302 156652 0 MC5R MC5 receptor Human 7.8 pEC50 = 7.8 ADMET
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 1511 43 21 17 -2.2 CC(C)C[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](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/acs.jmedchem.7b01295
CHEMBL602651 207910 0 MC5R MC5 receptor 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
CHEMBL4792291 182027 0 MC5R MC5 receptor 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 156722 0 MC5R MC5 receptor 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 156722 0 MC5R MC5 receptor 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 205212 0 MC5R MC5 receptor 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 94307 0 MC5R MC5 receptor 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 94307 0 MC5R MC5 receptor 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
137640475 156273 0 MC5R MC5 receptor 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 156273 0 MC5R MC5 receptor 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 194638 0 MC5R MC5 receptor 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 194638 0 MC5R MC5 receptor 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 190965 0 MC5R MC5 receptor 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 190965 0 MC5R MC5 receptor 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 94915 0 MC5R MC5 receptor 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 94915 0 MC5R MC5 receptor 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 207147 2 MC5R MC5 receptor 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 205340 0 MC5R MC5 receptor 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 205327 0 MC5R MC5 receptor 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 203685 0 MC5R MC5 receptor 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 155362 0 MC5R MC5 receptor 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 155362 0 MC5R MC5 receptor 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
CHEMBL1161321 202034 0 MC5R MC5 receptor 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
16132144 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 202802 28 MC5R MC5 receptor 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 207469 0 MC5R MC5 receptor 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 163216 0 MC5R MC5 receptor 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 163216 0 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 288 15 MC5R MC5 receptor 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 63773 0 MC5R MC5 receptor 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 63773 0 MC5R MC5 receptor 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]2Cc