GPCRdb

setmelanotide

Agent/drug
Bioactivity

setmelanotide

SMILES	None
InChIKey	HDHDTKMUACZDAA-PHNIDTBTSA-N
Sequence	RCAHFRWC

Chemical Properties

Hydrogen bond acceptors	None
Hydrogen bond donors	None
Rotatable bonds	None
Molecular weight (Da)

Database connections

PubChem Guide To Pharmacology Drug Central ChEMBL_compound_ids DrugBank PubChem GPCRdb
Structure pdb	7PIU 7AUE
Ligand site mutations	MC₄

Bioactivities

Affinity
Potency

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

MC₁	MSHR	Human	Melanocortin	A	pKi	8.41	8.41	8.41	Guide to Pharmacology
MC₁	MSHR	Human	Melanocortin	A	pKi	8.34	8.34	8.34	ChEMBL
MC₁	MSHR	Human	Melanocortin	A	pKi	8.08	8.08	8.08	Drug Central
MC₃	MC3R	Human	Melanocortin	A	pKi	8.00	8.00	8.00	Guide to Pharmacology
MC₃	MC3R	Human	Melanocortin	A	pKi	7.88	7.88	7.88	ChEMBL
MC₃	MC3R	Human	Melanocortin	A	pKi	8.10	8.10	8.10	Drug Central
MC₄	MC4R	Human	Melanocortin	A	pKi	8.68	8.68	8.68	Guide to Pharmacology
MC₄	MC4R	Rat	Melanocortin	A	pKi	8.57	8.57	8.57	Guide to Pharmacology
MC₄	MC4R	Human	Melanocortin	A	pKi	8.37	8.38	8.39	ChEMBL
MC₄	MC4R	Human	Melanocortin	A	pKd	8.06	8.06	8.06	Drug Central
MC₅	MC5R	Human	Melanocortin	A	pKi	6.37	6.37	6.37	Guide to Pharmacology
MC₅	MC5R	Human	Melanocortin	A	pKi	8.20	8.20	8.20	Drug Central

Showing 1 to 12 of 12 entries

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

MC₁	MSHR	Human	Melanocortin	A	pEC50	9.80	9.80	9.80	ChEMBL
MC₃	MC3R	Human	Melanocortin	A	pEC50	9.82	9.82	9.82	ChEMBL
MC₄	MC4R	Rat	Melanocortin	A	pEC50	9.55	9.55	9.55	ChEMBL
MC₄	MC4R	Human	Melanocortin	A	pEC50	9.40	9.46	9.57	ChEMBL
MC₅	MC5R	Human	Melanocortin	A	pIC50	5.72	5.72	5.73	ChEMBL

Showing 1 to 5 of 5 entries

setmelanotide

Drug properties

Molecular type	Peptide
Physiological/Surrogate	Surrogate
Approved drug	Yes

Distribution across phases (no. indications)

Phase I 1

Phase II 1

Phase III 0

Phase IV 2

Database connections

PubChem Guide To Pharmacology Drug Central ChEMBL_compound_ids DrugBank PubChem GPCRdb
Structure pdb	7PIU 7AUE
Ligand site mutations	MC₄

Sankey plot

Drug Information

Search:

Target					Disease

Gene	Protein	Receptor family	Ligand type	Class	Name	Phase	ICD11	ATC	Association score

MC4R	MC₄ receptor	Melanocortin receptors	Peptide receptors	A	Deletions of the short arm of chromosome 17	2	LD44.H1	A08A	0.008
MC4R	MC₄ receptor	Melanocortin receptors	Peptide receptors	A	Hypopituitarism	4	5A61.0	A08A	0.274
MC4R	MC₄ receptor	Melanocortin receptors	Peptide receptors	A	Obesity in adults	1	5B81.01	A08A	0.047
MC4R	MC₄ receptor	Melanocortin receptors	Peptide receptors	A	Obesity, unspecified	4	5B81.Z	A08A	0.804

Showing 1 to 4 of 4 entries