Compound Detail
CHEMBL1201185
LANREOTIDE 💊 Approved Drug
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💊 Approved Drug
CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O
Basic Information
| ChEMBL ID | CHEMBL1201185 |
| Name | LANREOTIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | PUDHBTGHUJUUFI-SCTWWAJVSA-N |
| Therapeutic | ✓ Yes |
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
5
Known Names
20
Indications
Molecular Properties
1096.3
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2007 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Acromegaly Carcinoid Heart Disease Carcinoid Tumor Carcinoid Tumor Endocrine Gland Neoplasms Malignant Carcinoid Syndrome Neoplasms Pituitary Neoplasms Polycystic Kidney, Autosomal Dominant Prostatic Neoplasms, Castration-Resistant Rectal Neoplasms Carcinoma, Hepatocellular Carcinoma, Merkel Cell Diarrhea Dumping Syndrome Esophagitis, Peptic Graves Ophthalmopathy Hyperglycemia Intestinal Diseases Intestinal Obstruction
ATC Classification
H01CB03
lanreotide
Level 1: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
Level 2: PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
Activity Summary
Ki 4 meas. best 9.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Somatostatin receptor type 2 CHEMBL1804 | Ki | 9.3 | 9.3 | 0.5 | 1 |
| Somatostatin receptor type 5 CHEMBL1792 | Ki | 8.4 | 8.4 | 4.0 | 1 |
| Somatostatin receptor type 3 CHEMBL2028 | Ki | 7.2 | 7.2 | 63.1 | 1 |
| Somatostatin receptor type 1 CHEMBL1917 | Ki | 6.3 | 6.3 | 501.2 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Somatostatin receptor type 2 | Ki | = | 0.5012 | nM | 9.3 | Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[... | 12773038 |
| Somatostatin receptor type 5 | Ki | = | 3.981 | nM | 8.4 | Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[... | 12773038 |
| Somatostatin receptor type 3 | Ki | = | 63.1 | nM | 7.2 | Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[... | 12773038 |
| Somatostatin receptor type 1 | Ki | = | 501.19 | nM | 6.3 | Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[... | 12773038 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | Unchecked | 11 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | NON-PROTEIN TARGET | 8 |
| 20014752 | 10.1021/tx900326k | Hepatotoxicity | 3 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 1 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 2 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 3 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 4 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 5 | 1 |
| 7783129 | 10.1021/jm00011a017 | Unchecked | 1 |
Data from ChEMBL 36 via Core Engine