nilotinib
Ligand Summary
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.
UNII: F41401512X
PubChem: 644241
Guide to Pharmacology: 5697
ChEMBL: CHEMBL255863
DrugCentral: 1932
LyCHI: HBA97ATR7TC8
Target Activities
ABL1
Tyrosine-protein kinase ABL1
22 Activities
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1 – 10 of 22
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 7.8 | |||||
IC50 | 8.92 | Bioorg Med Chem, (2020) 28:6:115344 | ||||
Kd | 8.44 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
Kd | 8.31 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.31 | J Med Chem, (2019) 62:22:10005 | ||||
IC50 | 8.26 | ACS Med Chem Lett, (2020) 11:4:491 | ||||
Kd | 8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.89 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
DDR2
Discoidin domain-containing receptor 2
7 Activities
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1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 9.3 | |||||
IC50 | 8.7 | J. Med. Chem., (2014) 57:10:4252 | ||||
IC50 | 8.28 | Bioorg. Med. Chem., (2010) 18:19:6977 | ||||
Kd | 8.22 | J. Med. Chem., (2014) 57:10:4252 | ||||
Kd | 8.21 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
IC50 | 7.75 | J. Med. Chem., (2014) 57:10:4252 | ||||
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) | ||
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IC50 | 7.37 | |||||
Kd | 8.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 8.43 | Bioorg. Med. Chem., (2010) 18:19:6977 | ||||
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) | ||
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IC50 | 7.83 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
Kd | 7.77 | Bioorg. Med. Chem. Lett., (2013) 23:3:682 | ||||
Kd | 7.66 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.54 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
2 Activities
KCNH2
Potassium voltage-gated channel subfamily H member 2
2 Activities
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) | ||
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Kd | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | |||||
NQO2
Ribosyldihydronicotinamide dehydrogenase [quinone]
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.42 | ACS Med Chem Lett, (2017) 8:2:215 | ||||
IC50 | 6.42 | |||||
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) | ||
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Kd | 7.58 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.59 | |||||
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) | ||
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Ki | 7 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA1
Carbonic anhydrase 1
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Ki | 7.53 | 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) | ||
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Ki | 8.39 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CYP3A4
Cytochrome P450 3A4
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.24 | ACS Med Chem Lett, (2020) 11:4:491 | ||||
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) | ||
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Ki | 6.52 | 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) | ||
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Ki | 6.35 | 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) | ||
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Ki | 6.34 | 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) | ||
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Ki | 6.65 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
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) | ||
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Ki | 7.38 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
CA4
Carbonic anhydrase 4
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Ki | 6.35 | Bioorg. Med. Chem. Lett., (2009) 19:15:4102 | ||||
BCR
Breakpoint cluster region protein
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 6.19 | Science, (2017) 358:6367:None | ||||
ILK
Integrin-linked protein kinase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 7.7 | Science, (2017) 358:6367:None | ||||