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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 28 hits in this display   

LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0790nMAssay 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
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0790nMAssay 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
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0790nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0900nMAssay 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
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0900nMAssay 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 3-kinase regulatory subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0900nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.120nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.290nMAssay 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
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.300nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.970nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  1.43nMAssay 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
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  1.43nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  9.10nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  23.7nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  23.7nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  53nMAssay 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
TargetPhosphatidylinositol 3-kinase regulatory subunit beta(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  53nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  1.20E+3nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50: <0.700nMAssay Description:Inhibition of PI3K delta (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50: <0.700nMAssay Description:Inhibition of PI3K alpha (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473More data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50:  31nMAssay Description:Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylationMore data for this Ligand-Target Pair
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50:  292nMAssay Description:Inhibition of PI3KC2beta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50:  374nMAssay Description:Inhibition of human VPS34More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDNA-dependent protein kinase catalytic subunit(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50: >4.80E+3nMAssay Description:Inhibition of DNA-dependent protein kinase (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PI3KC2alpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataEC50:  24nMAssay Description:Inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation after 24 hrs by electrochemiluminescent ...More data for this Ligand-Target Pair