Compound Detail
CHEMBL1201199
LEUPROLIDE 💊 Approved Drug
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💊 Approved Drug
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 | CHEMBL1201199 |
| Name | LEUPROLIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | GFIJNRVAKGFPGQ-LIJARHBVSA-N |
| Therapeutic | ✓ Yes |
3
Targets
9
Activities
2
Assay Types
12
PK Parameters
20
Publications
11
Known Names
20
Indications
Molecular Properties
1209.4
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 1985 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Neoplasms Breast Neoplasms Breast Neoplasms Endometriosis Infertility Leiomyoma Leiomyoma Myoma Pain Prostatic Neoplasms Prostatic Neoplasms Prostatic Neoplasms Prostatic Neoplasms, Castration-Resistant Hyperandrogenism Hypogonadism Liver Neoplasms Melanoma Salivary Gland Neoplasms HIV Infections Menopause
ATC Classification
L02AE02
leuprorelin
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ENDOCRINE THERAPY
Activity Summary
IC50 8 meas. best 9.54
Ki 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor CHEMBL1855 | IC50 | 9.54 | 9.42 | 0.3 | 4 |
| Gonadotropin-releasing hormone receptor CHEMBL3066 | IC50 | 9.3 | 9.2333 | 0.5 | 3 |
| Unchecked CHEMBL612545 | IC50 | 9.12 | 9.12 | 0.8 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 138.0 | ng.hr.mL-1 | Mus musculus |
| CL | 9.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 2.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.007 | ml/hr | Mus musculus |
| Cmax | 157.1 | nM | Mus musculus |
| Fu | 0.54 | - | Homo sapiens |
| MRT | 3.1 | hr | Homo sapiens |
| T1/2 | 0.01667 | hr | - |
| T1/2 | 0.06667 | hr | Rattus norvegicus |
| T1/2 | 2.9 | hr | Homo sapiens |
| T1/2 | 0.7 | hr | Mus musculus |
| Tmax | 1.0 | hr | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine