alpelisib
Alpelisib is an inhibitor of phosphatidylinositol-3- kinase (PI3K) with inhibitory activity predominantly against PI3Kalpha. Gain-of-function mutations in the gene encoding the catalytic alpha-subunit of PI3K (PIK3CA) lead to activation of PI3Kalpha and Akt-signaling, cellular transformation and the generation of tumors in in vitro and in vivo models.
Ligand Summary
UNII: 08W5N2C97Q
PubChem: 56649450
Guide to Pharmacology: 7955
ChEMBL: CHEMBL2396661
DrugCentral: 5328
LyCHI: DPT3VS8J5C2W
Target Activities
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PIK3CA
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
6 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.3 | Bioorg. Med. Chem. Lett., (2013) 23:13:3741 | ||||
IC50 | 8.3 | Bioorg. Med. Chem. Lett., (2015) 25:17:3582 | ||||
IC50 | 8.3 | Bioorg. Med. Chem. Lett., (2015) 25:17:3569 | ||||
IC50 | 8.34 | J Med Chem, (2017) 60:1:47 | ||||
IC50 | 8.30000019 | |||||
IC50 | 8.3372 | INHIBITOR | ||||
PIK3CB
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.92000008 | |||||
PIK3CD
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.53999996 | |||||
PIK3CG
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
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 | 6.5999999 | |||||