Compound Detail
CHEMBL3349607
PASIREOTIDE 💊 Approved Drug
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💊 Approved Drug
NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O
Basic Information
| ChEMBL ID | CHEMBL3349607 |
| Name | PASIREOTIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | VMZMNAABQBOLAK-DBILLSOUSA-N |
| Therapeutic | ✓ Yes |
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
6
Known Names
20
Indications
Molecular Properties
1047.2
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2012 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Acromegaly Carcinoid Tumor Carcinoid Tumor Pancreatic Neoplasms Pituitary ACTH Hypersecretion ACTH Syndrome, Ectopic Adenoma Adenoma, Islet Cell Breast Neoplasms Carcinoma, Hepatocellular Carcinoma, Medullary Cushing Syndrome Dumping Syndrome Hematologic Neoplasms Hyperglycemia Lung Neoplasms Meningioma Multiple Myeloma Neoplasms Neuroendocrine Tumors
ATC Classification
H01CB05
pasireotide
Level 1: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
Level 2: PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
Activity Summary
Ki 4 meas. best 9.9
IC50 1 meas. best 9.4
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Somatostatin receptor type 5 CHEMBL1792 | Ki | 9.9 | 9.9 | 0.1 | 1 |
| Rattus norvegicus CHEMBL376 | IC50 | 9.4 | 9.4 | 0.4 | 1 |
| Somatostatin receptor type 3 CHEMBL2028 | Ki | 9.1 | 9.1 | 0.8 | 1 |
| Somatostatin receptor type 2 CHEMBL1804 | Ki | 9.0 | 9.0 | 1.0 | 1 |
| Somatostatin receptor type 1 CHEMBL1917 | Ki | 8.2 | 8.2 | 6.3 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Somatostatin receptor type 5 | Ki | = | 0.1259 | nM | 9.9 | Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[... | 12773038 |
| Rattus norvegicus | IC50 | = | 0.4 | nM | 9.4 | In vitro inhibition of GHRH induced GH release in primary cultures of rat pituit... | 12773038 |
| Somatostatin receptor type 3 | Ki | = | 0.7943 | nM | 9.1 | Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[... | 12773038 |
| Somatostatin receptor type 2 | Ki | = | 1.0 | nM | 9.0 | Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[... | 12773038 |
| Somatostatin receptor type 1 | Ki | = | 6.31 | nM | 8.2 | Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[... | 12773038 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 37468498 | 10.1038/s41467-023-40064-9 | Cannabinoid receptor 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 6 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Histamine H1 receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Kappa-type opioid receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Substance-K receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(4) dopamine receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Neuronal acetylcholine receptor subunit alpha-4 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Beta-2 adrenergic receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Beta-1 adrenergic receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-dependent L-type calcium channel subunit alpha-1C | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 7 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 1 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Histamine H2 receptor | 1 |
| 12773038 | 10.1021/jm021093t | Rattus norvegicus | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 5 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 4 | 1 |
| 12773038 | 10.1021/jm021093t | Somatostatin receptor type 3 | 1 |
Data from ChEMBL 36 via Core Engine