Compound Detail
CHEMBL2105717
CABOZANTINIB 💊 Approved Drug
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💊 Approved Drug
COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC
Basic Information
| ChEMBL ID | CHEMBL2105717 |
| Name | CABOZANTINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ONIQOQHATWINJY-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
75
Targets
297
Activities
3
Assay Types
6
PK Parameters
20
Publications
3
Known Names
20
Indications
Molecular Properties
501.5
MW (Da)
5.54
ALogP
6
HBA
2
HBD
98.8
PSA (Ų)
0.31
QED
2
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2012 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Neoplasms Neoplasms Carcinoma, Hepatocellular Carcinoma, Medullary Carcinoma, Non-Small-Cell Lung Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Thyroid Neoplasms Thyroid Neoplasms Thyroid Neoplasms Adenocarcinoma, Follicular Adrenal Cortex Neoplasms Astrocytoma Bile Duct Neoplasms Breast Neoplasms
ATC Classification
L01EX07
cabozantinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 276 meas. best 10.46
Kd 20 meas. best 7.28
Ki 1 meas. best 10.46
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Vascular endothelial growth factor receptor 2 CHEMBL279 | Ki | 10.46 | 10.46 | 0.0 | 1 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 10.46 | 8.5921 | 0.0 | 33 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | IC50 | 9.22 | 7.6233 | 0.6 | 9 |
| BaF3 CHEMBL614524 | IC50 | 8.89 | 8.276 | 1.3 | 5 |
| SAFB-like transcription modulator CHEMBL4523469 | IC50 | 8.89 | 8.89 | 1.3 | 1 |
| Hepatocyte growth factor receptor CHEMBL3717 | IC50 | 8.89 | 7.8785 | 1.3 | 40 |
| Unchecked CHEMBL612545 | IC50 | 8.85 | 6.9557 | 1.4 | 7 |
| H-2 class II histocompatibility antigen gamma chain/Proto-oncogene tyrosine-protein kinase ROS CHEMBL6066844 | IC50 | 8.82 | 8.82 | 1.5 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | IC50 | 8.62 | 7.483 | 2.4 | 47 |
| MHCC97H CHEMBL4296470 | IC50 | 8.58 | 8.58 | 2.6 | 1 |
| Aurora kinase B/Receptor-type tyrosine-protein kinase CHEMBL3430908 | IC50 | 8.54 | 8.54 | 2.9 | 1 |
| Tyrosine-protein kinase receptor UFO CHEMBL4895 | IC50 | 8.47 | 7.9283 | 3.4 | 12 |
| Mast/stem cell growth factor receptor Kit CHEMBL1936 | IC50 | 8.4 | 7.828 | 4.0 | 10 |
| EBC-1 CHEMBL4296411 | IC50 | 8.32 | 7.5525 | 4.8 | 4 |
| Vascular endothelial growth factor receptor 3 CHEMBL1955 | IC50 | 8.22 | 8.22 | 6.0 | 1 |
| MKN-45 CHEMBL614354 | IC50 | 8.16 | 6.5033 | 6.9 | 3 |
| Hs746T CHEMBL614579 | IC50 | 8.0 | 8.0 | 9.9 | 1 |
| Fibroblast growth factor receptor 1 CHEMBL3650 | IC50 | 7.95 | 7.95 | 11.3 | 2 |
| HepG2 CHEMBL395 | IC50 | 7.92 | 5.63 | 12.0 | 5 |
| SNU-5 CHEMBL614934 | IC50 | 7.92 | 7.63 | 12.1 | 3 |
| Vascular endothelial growth factor receptor 1 CHEMBL1868 | IC50 | 7.92 | 7.92 | 12.0 | 2 |
| Angiopoietin-1 receptor CHEMBL4128 | IC50 | 7.84 | 7.84 | 14.3 | 5 |
| Epidermal growth factor receptor CHEMBL203 | IC50 | 7.72 | 6.6267 | 19.0 | 3 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 7.66 | 6.83 | 21.9 | 2 |
| HEK293 CHEMBL614818 | IC50 | 7.57 | 6.5433 | 27.0 | 3 |
| Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET CHEMBL3430904 | IC50 | 7.47 | 6.76 | 34.0 | 2 |
| NCI-H460 CHEMBL396 | IC50 | 7.4 | 6.03 | 40.1 | 3 |
| HUVEC CHEMBL613979 | IC50 | 7.35 | 6.235 | 45.0 | 2 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | Kd | 7.28 | 7.28 | 53.0 | 1 |
| Macrophage-stimulating protein receptor CHEMBL2689 | IC50 | 7.16 | 7.035 | 69.0 | 2 |
| High affinity nerve growth factor receptor CHEMBL2815 | IC50 | 7.14 | 7.12 | 72.3 | 2 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 7.07 | 7.07 | 86.0 | 1 |
| NCI-H1993 CHEMBL1075527 | IC50 | 6.96 | 6.96 | 110.0 | 1 |
| Proto-oncogene tyrosine-protein kinase Src CHEMBL267 | IC50 | 6.75 | 6.75 | 178.0 | 1 |
| Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET CHEMBL3430888 | IC50 | 6.72 | 6.72 | 190.0 | 1 |
| Epithelial discoidin domain-containing receptor 1 CHEMBL5319 | Kd | 6.68 | 6.68 | 209.0 | 1 |
| HeLa CHEMBL399 | IC50 | 6.5 | 5.51 | 320.0 | 3 |
| A549 CHEMBL392 | IC50 | 6.48 | 5.4155 | 330.0 | 11 |
| Breakpoint cluster region protein CHEMBL5146 | Kd | 6.47 | 6.47 | 342.0 | 1 |
| MCF7 CHEMBL387 | IC50 | 6.35 | 5.3644 | 450.0 | 9 |
| Discoidin domain-containing receptor 2 CHEMBL5122 | Kd | 6.3 | 6.3 | 501.0 | 1 |
| Tyrosine-protein kinase FRK CHEMBL4223 | Kd | 6.25 | 6.25 | 560.0 | 1 |
| Ephrin type-A receptor 2 CHEMBL2068 | Kd | 6.13 | 6.13 | 746.0 | 1 |
| Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014 | Kd | 6.12 | 6.12 | 767.0 | 1 |
| Tyrosine-protein kinase ABL2 CHEMBL4014 | Kd | 6.04 | 6.04 | 918.0 | 1 |
| Tyrosine-protein kinase Lck CHEMBL258 | Kd | 5.98 | 5.98 | 1045.0 | 1 |
| Tyrosine-protein kinase ABL1 CHEMBL1862 | Kd | 5.96 | 5.96 | 1098.0 | 1 |
| Tyrosine-protein kinase HCK CHEMBL3234 | Kd | 5.96 | 5.96 | 1098.0 | 1 |
| Tyrosine-protein kinase Lyn CHEMBL3905 | Kd | 5.88 | 5.88 | 1333.0 | 1 |
| CAKI-1 CHEMBL614067 | IC50 | 5.78 | 5.78 | 1660.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 3.16 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 6.76 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| Cmax | 1104.66 | nM | Homo sapiens |
| t1/2 | - | - | Homo sapiens |
| T1/2 | 112.0 | hr | Homo sapiens |
| Tmax | 4.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine