Compile Data Set for Download or QSAR
maximum 50k data
Found 34 Enz. Inhib. hit(s) with Target = 'Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform' and Ligand = 'BDBM25028'
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails US Patent
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of p110alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant PI3Kalpha assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of human PI3Kalpha incubated for 1 hr by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  6nMMore data for this Ligand-Target Pair
In DepthDetails
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  7nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  33nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  0.860nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  1.70nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  4.10nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  1.20nMAssay Description:Binding constant for PIK3CA(E545K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  7.10nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  1.10nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  4.5nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  3.70nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
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
In DepthDetails ArticlePubMed