copanlisib
Ligand Summary
Copanlisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells. Copanlisib has been shown to induce tumor cell death by apoptosis and inhibition of proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell-signaling pathways, including B-cell receptor (BCR) signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFkB signaling in lymphoma cell lines.
UNII: WI6V529FZ9
ChEMBL: CHEMBL3218576
DrugCentral: 5256
LyCHI: H3234GC54PVS
Target Activities
PIK3CB
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
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 | Eur J Med Chem, (2016) 122:None:731 | ||||
IC50 | 8.43 | Eur J Med Chem, (2019) 183:None:111718 | ||||
IC50 | 8.43 | J Med Chem, (2019) 62:10:4815 | ||||
IC50 | 8.43 | INHIBITOR | ||||
PIK3CA
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 9.3 | Eur J Med Chem, (2016) 122:None:731 | ||||
IC50 | 9.3 | Eur J Med Chem, (2019) 183:None:111718 | ||||
IC50 | 9.3 | J Med Chem, (2019) 62:10:4815 | ||||
IC50 | 9.3 | INHIBITOR | ||||
PIK3CG
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 9.15 | Eur J Med Chem, (2019) 183:None:111718 | ||||
IC50 | 8.78 | J Med Chem, (2020) 63:6:3028 | ||||
IC50 | 8.19 | Eur J Med Chem, (2016) 122:None:731 | ||||
IC50 | 8.19 | J Med Chem, (2019) 62:10:4815 | ||||
PIK3CD
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 9.15 | Eur J Med Chem, (2016) 122:None:731 | ||||
IC50 | 8.19 | Eur J Med Chem, (2019) 183:None:111718 | ||||
IC50 | 9.15 | INHIBITOR | ||||