Compound Detail
CHEMBL2070241
BREMELANOTIDE 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)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
Basic Information
| ChEMBL ID | CHEMBL2070241 |
| Name | BREMELANOTIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | FFHBJDQSGDNCIV-MFVUMRCOSA-N |
| Therapeutic | ✓ Yes |
4
Targets
28
Activities
3
Assay Types
1
PK Parameters
20
Publications
4
Known Names
3
Indications
1
Mechanisms
Molecular Properties
1025.2
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2019 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Melanocortin receptor 4 agonist | AGONIST | Melanocortin receptor 4 | ✓ | ✓ |
Indications
Sexual Dysfunction, Physiological Kidney Diseases Nausea
ATC Classification
G02CX05
bremelanotide
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: OTHER GYNECOLOGICALS
Activity Summary
Ki 13 meas. best 9.6
EC50 12 meas. best 10.11
IC50 3 meas. best 6.71
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Melanocyte-stimulating hormone receptor CHEMBL3795 | EC50 | 10.11 | 10.08 | 0.1 | 3 |
| Melanocortin receptor 4 CHEMBL259 | EC50 | 9.92 | 9.2167 | 0.1 | 6 |
| Melanocortin receptor 4 CHEMBL259 | Ki | 9.6 | 8.1425 | 0.2 | 4 |
| Melanocortin receptor 3 CHEMBL4644 | EC50 | 9.17 | 8.9867 | 0.7 | 3 |
| Melanocyte-stimulating hormone receptor CHEMBL3795 | Ki | 8.72 | 8.5875 | 1.9 | 4 |
| Melanocortin receptor 5 CHEMBL4608 | Ki | 7.77 | 7.77 | 17.0 | 1 |
| Melanocortin receptor 3 CHEMBL4644 | Ki | 7.28 | 6.85 | 53.0 | 4 |
| Melanocortin receptor 5 CHEMBL4608 | IC50 | 6.71 | 6.7033 | 195.0 | 3 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| T1/2 | 2.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine