Compound Detail
CHEMBL1200775
LEUPROLIDE ACETATE 💊 Approved Drug
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💊 Approved Drug
CC(=O)O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1
Basic Information
| ChEMBL ID | CHEMBL1200775 |
| Name | LEUPROLIDE ACETATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RGLRXNKKBLIBQS-XNHQSDQCSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL1201199 |
| Active Moiety | CHEMBL1201199 |
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
27
Known Names
20
Indications
1
Mechanisms
Molecular Properties
1209.4
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 1985 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor agonist | AGONIST | Gonadotropin-releasing hormone receptor | ✓ | ✓ |
Indications
Prostatic Neoplasms Prostatic Neoplasms Prostatic Neoplasms Prostatic Neoplasms Puberty, Precocious Puberty, Precocious Breast Neoplasms Breast Neoplasms Endometriosis Infertility, Male Leiomyoma Neoplasms Obesity Alzheimer Disease Bulimia Nervosa Cognitive Dysfunction Depression, Postpartum Depressive Disorder Granulosa Cell Tumor Hodgkin Disease
Activity Summary
IC50 1 meas. best 4.1
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 2 CHEMBL5748 | IC50 | 4.1 | 4.1 | 80200.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 2 | IC50 | = | 80200.0 | nM | 4.1 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as... | 23956101 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 24047141 | 10.1021/jm401056w | Rattus norvegicus | 1 |
| 23956101 | 10.1093/toxsci/kft176 | Bile salt export pump | 1 |
| 23956101 | 10.1093/toxsci/kft176 | ATP-binding cassette sub-family C member 2 | 1 |
| 23956101 | 10.1093/toxsci/kft176 | ATP-binding cassette sub-family C member 3 | 1 |
| 23956101 | 10.1093/toxsci/kft176 | ATP-binding cassette sub-family C member 4 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine