Compound Detail
CHEMBL1567
SUNITINIB MALATE 💊 Approved Drug
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💊 Approved Drug
CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C.O=C(O)C[C@H](O)C(=O)O
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
8
Known Names
20
Indications
6
Mechanisms
Molecular Properties
398.5
MW (Da)
3.33
ALogP
3
HBA
3
HBD
77.2
PSA (Ų)
0.63
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2006 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Macrophage colony stimulating factor receptor inhibitor | INHIBITOR | Macrophage colony-stimulating factor 1 receptor | ✓ | ✓ |
| Stem cell growth factor receptor inhibitor | INHIBITOR | Mast/stem cell growth factor receptor Kit | ✓ | ✓ |
| Tyrosine-protein kinase receptor FLT3 inhibitor | INHIBITOR | Receptor-type tyrosine-protein kinase FLT3 | ✓ | ✓ |
| Platelet-derived growth factor receptor inhibitor | INHIBITOR | Platelet-derived growth factor receptor | ✓ | ✓ |
| Vascular endothelial growth factor receptor inhibitor | INHIBITOR | Vascular endothelial growth factor receptor | ✓ | ✓ |
| Tyrosine-protein kinase receptor RET inhibitor | INHIBITOR | Proto-oncogene tyrosine-protein kinase receptor Ret | ✓ | ✓ |
Indications
Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Gastrointestinal Stromal Tumors Neuroendocrine Tumors Breast Neoplasms Breast Neoplasms Carcinoma, Hepatocellular Carcinoma, Islet Cell Carcinoma, Non-Small-Cell Lung Kidney Neoplasms Kidney Neoplasms Pancreatic Neoplasms Adenocarcinoma, Follicular Adenoma, Islet Cell Astrocytoma Astrocytoma Breast Neoplasms, Male Carcinoma, Medullary Carcinoma, Ovarian Epithelial
Drug Warnings
Black Box Warning
hepatotoxicity
Black Box Warning
hematological toxicity
Activity Summary
IC50 4 meas. best 8.7
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Platelet-derived growth factor receptor beta CHEMBL1913 | IC50 | 8.7 | 8.7 | 2.0 | 1 |
| Macrophage colony-stimulating factor 1 receptor CHEMBL1844 | IC50 | 7.92 | 7.92 | 12.0 | 1 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 7.1 | 7.1 | 80.0 | 1 |
| ACHN CHEMBL614519 | IC50 | 5.7 | 5.7 | 2000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Platelet-derived growth factor receptor beta | IC50 | = | 2.0 | nM | 8.7 | Inhibition of PDGFRbeta (unknown origin) by enzymatic assay | 37944387 |
| Macrophage colony-stimulating factor 1 receptor | IC50 | = | 12.0 | nM | 7.92 | Inhibition of CSF1R | 18694641 |
| Vascular endothelial growth factor receptor 2 | IC50 | = | 80.0 | nM | 7.1 | Inhibition of VEGFR2 (unknown origin) | 37944387 |
| ACHN | IC50 | = | 2000.0 | nM | 5.7 | Cytotoxicity against human ACHN cells after 72 hrs by MTT assay | 25124114 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 24894557 | 10.1016/j.bmcl.2014.05.005 | Chorioallantoic membrane | 2 |
| 18694641 | 10.1016/j.bmcl.2008.07.093 | Macrophage colony-stimulating factor 1 receptor | 1 |
| 18694641 | 10.1016/j.bmcl.2008.07.093 | NIH3T3 | 1 |
| 25124114 | 10.1016/j.bmcl.2014.07.066 | ACHN | 1 |
| 37944387 | 10.1016/j.ejmech.2023.115928 | Vascular endothelial growth factor receptor 2 | 1 |
| 37944387 | 10.1016/j.ejmech.2023.115928 | Platelet-derived growth factor receptor beta | 1 |
| 38157838 | 10.1016/j.bmc.2023.117561 | Unchecked | 1 |
Data from ChEMBL 36 via Core Engine