entrectinib
Ligand Summary
Entrectinib is an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK).
UNII: L5ORF0AN1I
PubChem: 25141092
ChEMBL: CHEMBL1983268
DrugCentral: 5345
LyCHI: SQPN7K5NY3NW
Target Activities
NTRK1
High affinity nerve growth factor receptor
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.66 | Bioorg Med Chem Lett, (2019) 29:19:126624 | ||||
IC50 | 9 | J. Med. Chem., (2016) 59:7:3392 | ||||
Ki | 8.8 | None, None:None:None | ||||
Kd | 8.7 | Science, (2017) 358:6367:None | ||||
IC50 | 8.54 | Bioorg Med Chem Lett, (2019) 29:19:126624 | ||||
IC50 | 8.52 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 9 | INHIBITOR | ||||
ALK
ALK tyrosine kinase receptor
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9 | None, None:None:None | ||||
Ki | 8.21 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 7.92 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 7.92 | Eur J Med Chem, (2018) 143:None:182 | ||||
IC50 | 7.92 | INHIBITOR | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.3 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.15 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.15 | Eur J Med Chem, (2018) 143:None:182 | ||||
IC50 | 8.15 | INHIBITOR | ||||
NTRK3
NT-3 growth factor receptor
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.8 | None, None:None:None | ||||
IC50 | 8.52 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.3 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.3 | INHIBITOR | ||||
NTRK2
BDNF/NT-3 growth factors receptor
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.6 | None, None:None:None | ||||
IC50 | 8.52 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.52 | J. Med. Chem., (2016) 59:7:3392 | ||||
IC50 | 8.52 | INHIBITOR | ||||
JAK2
Tyrosine-protein kinase JAK2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.7 | None, None:None:None | ||||
FER
Tyrosine-protein kinase Fer
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.3 | None, None:None:None | ||||
FRK
Tyrosine-protein kinase FRK
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.8 | None, None:None:None | ||||
LTK
Leukocyte tyrosine kinase receptor
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.8 | None, None:None:None | ||||