crizotinib
Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.
Ligand Summary
UNII: 53AH36668S
PubChem: 11626560
Guide to Pharmacology: 4903
ChEMBL: CHEMBL601719
DrugCentral: 4187
LyCHI: C52GL3ADX4W8
Target Activities
MET
Hepatocyte growth factor receptor
39 Activities
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1 – 10 of 39
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.1 | |||||
Ki | 8.7 | |||||
Kd | 9.7 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
IC50 | 9.29 | J Med Chem, (2019) 62:24:10927 | ||||
Kd | 9.26 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 9.11 | Bioorg. Med. Chem. Lett., (2011) 21:15:4592 | ||||
IC50 | 9.05 | Eur. J. Med. Chem., (2016) 115:None:191 | ||||
IC50 | 9.05 | Bioorg Med Chem Lett, (2020) 30:13:127189 | ||||
IC50 | 8.98 | Eur J Med Chem, (2018) 143:None:491 | ||||
IC50 | 8.96 | Bioorg. Med. Chem., (2013) 21:21:6804 | ||||
ALK
ALK tyrosine kinase receptor
31 Activities
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1 – 10 of 31
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9 | |||||
EC50 | 9.33 | MedChemComm, (2017) 8:10:1914 | ||||
IC50 | 9.19 | J. Med. Chem., (2016) 59:10:4948 | ||||
Ki | 9.13 | J. Med. Chem., (2014) 57:11:4720 | ||||
Ki | 9.13 | Eur J Med Chem, (2017) 134:None:348 | ||||
IC50 | 8.74 | J Med Chem, (2019) 62:10:4915 | ||||
IC50 | 8.68 | None, (2016) None:None:None | ||||
IC50 | 8.57 | None, (2016) None:None:None | ||||
IC50 | 8.54 | None, (2016) None:None:None | ||||
Kd | 8.52 | Science, (2017) 358:6367:None | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
9 Activities
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1 – 9 of 9
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.22 | Eur J Med Chem, (2017) 134:None:348 | ||||
IC50 | 9.15 | Eur. J. Med. Chem., (2015) 90:None:195 | ||||
Kd | 8.39 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8.24 | Eur J Med Chem, (2017) 134:None:348 | ||||
IC50 | 8.19 | Eur J Med Chem, (2016) 123:None:80 | ||||
IC50 | 8.19 | Eur J Med Chem, (2019) 183:None:111734 | ||||
IC50 | 8.17 | Eur J Med Chem, (2018) 143:None:123 | ||||
IC50 | 8.15 | MedChemComm, (2017) 8:3:621 | ||||
IC50 | 8.03 | Eur J Med Chem, (2019) 171:None:297 | ||||
ABL1
Tyrosine-protein kinase ABL1
3 Activities
MST1R
Macrophage-stimulating protein receptor
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | |||||
JAK2
Tyrosine-protein kinase JAK2
2 Activities
SLK
STE20-like serine/threonine-protein kinase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.75 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.74 | |||||
AXL
Tyrosine-protein kinase receptor UFO
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.11 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.11 | |||||
MERTK
Tyrosine-protein kinase Mer
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.44 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.44 | |||||
EPHB6
Ephrin type-B receptor 6
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.22 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.22 | |||||
LTK
Leukocyte tyrosine kinase receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
TEK
Angiopoietin-1 receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.3 | J. Med. Chem., (2011) 54:18:6342 | ||||
NTRK2
BDNF/NT-3 growth factors receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.7 | J. Med. Chem., (2011) 54:18:6342 | ||||
IRAK3
Interleukin-1 receptor-associated kinase 3
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.51 | |||||