nilotinib
Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
Ligand Summary
UNII: F41401512X
PubChem: 644241
Guide to Pharmacology: 5697
ChEMBL: CHEMBL255863
DrugCentral: 1932
LyCHI: HBA97ATR7TC8
Target Activities
ABL1
Tyrosine-protein kinase ABL1
19 Activities
Items per page:
1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.55 | Nat Rev Drug Discov, (2017) 16:6:424 | ||||
IC50 | 7.56 | J. Med. Chem., (2013) 56:3:879 | ||||
IC50 | 7.62 | J. Med. Chem., (2013) 56:3:879 | ||||
Kd | 7.68 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.68 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.75 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.8 | J. Med. Chem., (2013) 56:3:879 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.85 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
DDR2
Discoidin domain-containing receptor 2
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.21 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
Kd | 8.22 | J. Med. Chem., (2014) 57:10:4252 | ||||
IC50 | 8.28 | Bioorg. Med. Chem., (2010) 18:19:6977 | ||||
IC50 | 8.7 | J. Med. Chem., (2014) 57:10:4252 | ||||
IC50 | 9.30000019 | |||||
Kd | 8.22 | |||||
DDR1
Epithelial discoidin domain-containing receptor 1
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.43 | Bioorg. Med. Chem., (2010) 18:19:6977 | ||||
Kd | 8.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.36999989 | |||||
Kd | 8.96 | |||||
KIT
Mast/stem cell growth factor receptor Kit
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.54 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.77 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
IC50 | 7.83 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
ABL2
Tyrosine-protein kinase ABL2
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 | 7.58 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.59 | |||||
MAP3K20
Mitogen-activated protein kinase kinase kinase 20
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 | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | |||||
CA9
Carbonic anhydrase 9
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 | 7.38 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA3
Carbonic anhydrase 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) | ||
|---|---|---|---|---|---|---|
Ki | 6.35 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA14
Carbonic anhydrase 14
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 | 6.65 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA7
Carbonic anhydrase 7
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 | 7 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
NQO2
Ribosyldihydronicotinamide dehydrogenase [quinone]
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 | 6.42 | ACS Med Chem Lett, (2017) 8:2:215 | ||||
CA12
Carbonic anhydrase 12
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 | 6.52 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA2
Carbonic anhydrase 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) | ||
|---|---|---|---|---|---|---|
Ki | 8.39 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA1
Carbonic anhydrase 1
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 | 7.53 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA6
Carbonic anhydrase 6
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 | 6.34 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
CA4
Carbonic anhydrase 4
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.35 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||