ceritinib
Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays.
Ligand Summary
UNII: K418KG2GET
PubChem: 57379345
Guide to Pharmacology: 7397
ChEMBL: CHEMBL2403108
DrugCentral: 4866
LyCHI: BD9867SAV79T
Target Activities
ALK
ALK tyrosine kinase receptor
33 Activities
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1 – 10 of 33
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.7 | |||||
IC50 | 9.7 | J. Med. Chem., (2013) 56:14:5673 | ||||
IC50 | 9.7 | J. Med. Chem., (2013) 56:14:5675 | ||||
Kd | 8.89 | Eur J Med Chem, (2018) 151:None:304 | ||||
IC50 | 8.85 | Eur J Med Chem, (2017) 126:None:536 | ||||
IC50 | 8.82 | Eur J Med Chem, (2017) 126:None:536 | ||||
IC50 | 8.7 | Eur J Med Chem, (2017) 126:None:536 | ||||
IC50 | 8.7 | Eur J Med Chem, (2019) 171:None:297 | ||||
IC50 | 8.66 | J. Med. Chem., (2013) 56:14:5675 | ||||
IC50 | 8.64 | Eur J Med Chem, (2016) 123:None:80 | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.4 | Eur J Med Chem, (2017) 134:None:348 | ||||
Ki | 9.15 | Eur J Med Chem, (2017) 134:None:348 | ||||
IC50 | 8.7 | Eur J Med Chem, (2016) 123:None:80 | ||||
IC50 | 8.7 | Eur J Med Chem, (2018) 143:None:123 | ||||
IC50 | 8.51 | Eur J Med Chem, (2019) 171:None:297 | ||||
IC50 | 8.37 | Bioorg Med Chem, (2019) 27:20:115051 | ||||
INSR
Insulin receptor
3 Activities
TSSK1B
Testis-specific serine/threonine-protein kinase 1
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.64 | |||||
IC50 | 7.64 | J. Med. Chem., (2013) 56:14:5675 | ||||
IC50 | 7.64 | |||||
IGF1R
Insulin-like growth factor 1 receptor
2 Activities
EGFR
Epidermal growth factor receptor
2 Activities
ABCB1
Multidrug resistance protein 1
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 7.05 | Eur J Med Chem, (2019) 164:None:193 | ||||
EC50 | 7.05 | |||||
FLT3
Receptor-type tyrosine-protein kinase FLT3
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 | 7.22 | |||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
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 | 5.9 | J. Med. Chem., (2013) 56:14:5675 | ||||
TNK1
Non-receptor tyrosine-protein kinase TNK1
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 | 7.57 | Science, (2017) 358:6367:None | ||||