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Compound Detail

CHEMBL3301624

SETMELANOTIDE
💊 Approved Drug
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💊 Approved Drug
CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3301624
Name SETMELANOTIDE
Phase Approved
Structure Type BOTH
InChI Key HDHDTKMUACZDAA-PHNIDTBTSA-N
Therapeutic ✓ Yes

Known Names

BIM-22493 Imcivree RM-493 Setmelanotida Setmelanotide
5
Targets
16
Activities
3
Assay Types
1
PK Parameters
15
Publications
5
Known Names
5
Indications
1
Mechanisms

Molecular Properties

1117.3
MW (Da)

Drug Information

Molecule Type Protein
First Approval 2020
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Parenteral

Flags

Natural Product First in Class
USAN Stem -tide
USAN Year 2014

Extended Properties

Molecular Formula C49H68N18O9S2
MW 1117.33

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Melanocortin receptor 4 agonist AGONIST Melanocortin receptor 4 ✓ ✓

Indications

Obesity Bardet-Biedl Syndrome Prader-Willi Syndrome Obesity, Morbid Renal Insufficiency

ATC Classification

A08AA12
setmelanotide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS

Activity Summary

EC50 8 meas. best 9.82
Ki 6 meas. best 8.39
IC50 2 meas. best 5.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 3
CHEMBL4644
 EC50 9.82 9.82 0.2 2
Melanocyte-stimulating hormone receptor
CHEMBL3795
 EC50 9.8 9.8 0.2 2
Melanocortin receptor 4
CHEMBL259
 EC50 9.57 9.46 0.3 3
Melanocortin receptor 4
CHEMBL2700
 EC50 9.55 9.55 0.3 1
Melanocortin receptor 4
CHEMBL259
 Ki 8.39 8.38 4.1 2
Melanocyte-stimulating hormone receptor
CHEMBL3795
 Ki 8.34 8.34 4.6 2
Melanocortin receptor 3
CHEMBL4644
 Ki 7.88 7.88 13.2 2
Melanocortin receptor 5
CHEMBL4608
 IC50 5.73 5.725 1862.1 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 11.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 3 EC50 = 0.1514 nM 9.82 Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 c... 34197114
Melanocortin receptor 3 EC50 = 0.1514 nM 9.82 Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP prod... 36167503
Melanocyte-stimulating hormone receptor EC50 = 0.1585 nM 9.8 Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 c... 34197114
Melanocyte-stimulating hormone receptor EC50 = 0.1585 nM 9.8 Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP prod... 36167503
Melanocortin receptor 4 EC50 = 0.27 nM 9.57 Inhibition of human MC4R 36155354
Melanocortin receptor 4 EC50 = 0.28 nM 9.55 Inhibition of rat MC4R 36155354
Melanocortin receptor 4 EC50 = 0.389 nM 9.41 Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 c... 34197114
Melanocortin receptor 4 EC50 = 0.3981 nM 9.4 Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP p... 36167503
Melanocortin receptor 4 Ki = 4.074 nM 8.39 Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell ... 34197114
Melanocortin receptor 4 Ki = 4.266 nM 8.37 Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell ... 36167503
Melanocyte-stimulating hormone receptor Ki = 4.571 nM 8.34 Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell ... 34197114
Melanocyte-stimulating hormone receptor Ki = 4.571 nM 8.34 Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell ... 36167503
Melanocortin receptor 3 Ki = 13.18 nM 7.88 Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell ... 34197114
Melanocortin receptor 3 Ki = 13.18 nM 7.88 Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell ... 36167503
Melanocortin receptor 5 IC50 = 1862.09 nM 5.73 Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP prod... 36167503
Melanocortin receptor 5 IC50 = 1905.46 nM 5.72 Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell ... 34197114

Literature References

PubMed DOI Target Context # Activities
36167503 10.1021/acs.jmedchem.2c00793 Unchecked 4
34197114 10.1021/acs.jmedchem.1c00095 Melanocortin receptor 4 3
38345933 10.1021/acs.jmedchem.3c01822 Melanocortin receptor 4 3
34197114 10.1021/acs.jmedchem.1c00095 Melanocyte-stimulating hormone receptor 2
34197114 10.1021/acs.jmedchem.1c00095 Melanocortin receptor 3 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocyte-stimulating hormone receptor 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 3 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 4 2
36155354 10.1016/j.ejmech.2022.114742 Melanocortin receptor 4 2
38691890 10.1016/j.ejmech.2024.116456 ADMET 2
34197114 10.1021/acs.jmedchem.1c00095 Melanocortin receptor 5 1
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 5 1
35404053 10.1021/acs.jmedchem.1c01295 Melanocortin receptor 3 1
35404053 10.1021/acs.jmedchem.1c01295 Melanocortin receptor 4 1
38345933 10.1021/acs.jmedchem.3c01822 Unchecked 1

Data from ChEMBL 36 via Core Engine