zanubrutinib
BRUKINSA (zanubrutinib) is a Bruton’s tyrosine kinase (BTK) inhibitor. Zanubrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. In B-cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. In nonclinical studies, zanubrutinib inhibited malignant B-cell proliferation and reduced tumor growth.
Ligand Summary
UNII: AG9MHG098Z
PubChem: 135565884
PubChem: 121413432
Guide to Pharmacology: 9861
ChEMBL: CHEMBL3936761
DrugCentral: 5353
LyCHI: 15WQ7TBBGQZU
Target Activities
BTK
Tyrosine-protein kinase BTK
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.7 | |||||
IC50 | 9.52 | J Med Chem, (2019) 62:17:7923 | ||||
IC50 | 9.04 | J Med Chem, (2019) 62:17:7923 | ||||
IC50 | 8.74 | J Med Chem, (2019) 62:17:7923 | ||||
IC50 | 8.7 | None, (2016) None:None:None | ||||
IC50 | 9.52 | INHIBITOR | ||||
BLK
Tyrosine-protein kinase Blk
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 | 8.95 | J Med Chem, (2019) 62:17:7923 | ||||
EGFR
Epidermal growth factor 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) | ||
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IC50 | 8.59 | J Med Chem, (2019) 62:17:7923 | ||||
BMX
Cytoplasmic tyrosine-protein kinase BMX
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 | 9.21 | J Med Chem, (2019) 62:17:7923 | ||||
TEC
Tyrosine-protein kinase Tec
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 | 8.7 | J Med Chem, (2019) 62:17:7923 | ||||
TXK
Tyrosine-protein kinase TXK
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 | 8.53 | J Med Chem, (2019) 62:17:7923 | ||||
ERBB4
Receptor tyrosine-protein kinase erbB-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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IC50 | 8.8 | J Med Chem, (2019) 62:17:7923 | ||||