Found 34 Enz. Inhib. hit(s) with Target = 'Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform' and Ligand = 'BDBM25028'
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 2.56nMAssay Description:The biochemical inhibition of four PI3K isoforms by the Formula I compounds of Table 1. In addition, two clinically tested PI3K compounds, taselisib ...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 2.60nMAssay Description:Inhibition of GST-fused human recombinant PI3Kalpha expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 0.100nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of p110alphaMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha assessed as inhibition of PIP3 production for 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3K subunit p110alpha assessed as formation of phosphatidylinositide-3-phosphate product formation after 30 mins by fluorescence polar...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha assessed as reduction in 3,4,5-inositoltriphosphate accumulation after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant PI3Kalpha assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PI substrate incubated for 60 mins by kinase-glo luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate incubated for 60 mins by Kinase-Glo luminescent kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using poly (Glu, Tyr) 4:1 substrate incubated for 30 mins by HTRF assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 3nMAssay Description:Inhibition of purified PI3Kalpha (unknown origin) after 30 mins by homogeneous time-resolved fluorescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 4.70nMAssay Description:Inhibition of human PI3Kalpha incubated for 1 hr by ADP-Glo kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 6nMAssay Description:Inhibition of PI3Kalpha (unknown origin) by kinase-glo luminescent assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 6.5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in p...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 7nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 7nMAssay Description:Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 33nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 50nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in pr...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 52nMAssay Description:Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 251nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 251nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 0.860nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 1.70nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 4.10nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 1.20nMAssay Description:Binding constant for PIK3CA(E545K) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 1.5nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 7.10nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 1.10nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 4.5nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 3.70nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 1.5nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 0.760nMAssay Description:Binding affinity to human PI3Kalpha (R108 to N1068 residues) expressed in mammalian expression system by Kinomescan assayMore data for this Ligand-Target Pair