Compound Detail
CHEMBL5314377
GANIRELIX ACETATE 💊 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
CC(=O)O.CC(=O)O.CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O
Basic Information
| ChEMBL ID | CHEMBL5314377 |
| Name | GANIRELIX ACETATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OVBICQMTCPFEBS-SATRDZAXSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL1251 |
| Active Moiety | CHEMBL1251 |
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
6
Known Names
6
Indications
1
Mechanisms
Molecular Properties
1570.3
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 1999 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor antagonist | ANTAGONIST | Gonadotropin-releasing hormone receptor | ✓ | ✓ |
Indications
Infertility, Female Ovulation Induction Reproductive Techniques, Assisted Orthostatic Intolerance Cerebral Arterial Diseases Polycystic Ovary Syndrome
Activity Summary
IC50 1 meas. best 8.44
Kd 1 meas. best 9.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor CHEMBL1855 | Kd | 9.3 | 9.3 | 0.5 | 1 |
| Gonadotropin-releasing hormone receptor CHEMBL1855 | IC50 | 8.44 | 8.44 | 3.6 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | Kd | = | 0.5012 | nM | 9.3 | Competitive antagonism of GnRH-induced response in the reporter gene assay | 11462984 |
| Gonadotropin-releasing hormone receptor | IC50 | = | 3.6 | nM | 8.44 | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293... | 11462984 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 11462984 | 10.1021/jm0003900 | Rattus norvegicus | 5 |
| 11462984 | 10.1021/jm0003900 | Gonadotropin-releasing hormone receptor | 2 |
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
Data from ChEMBL 36 via Core Engine