BDBM25028 4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine::GDC-0941::GDC0941::US10112932, pictilisib::US10851091, Compound pictilisib

SMILES CS(=O)(=O)N1CCN(Cc2cc3nc(nc(N4CCOCC4)c3s2)-c2cccc3[nH]ncc23)CC1

InChI Key InChIKey=LHNIIDJUOCFXAP-UHFFFAOYSA-N

Data  14 KI  99 IC50  450 Kd  1 EC50

PDB links: 3 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 57 hits for monomerid = 25028   

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  1.54nMAssay 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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  1.54nMAssay 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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  31nMAssay Description:Inhibition of GST-fused human recombinant PI3Kdelta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  41.8nMAssay 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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  41.8nMAssay 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 beta(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  70.2nMAssay 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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  70.2nMAssay 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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  33nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  75nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  42nMAssay Description:Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  7nMAssay Description:Inhibition of human PI3KCdelta by non-radiometric ADP-Glo assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  66nMAssay Description:Inhibition of recombinant PI3Kgamma assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant PI3Kdelta assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  32nMAssay Description:Inhibition of recombinant PI3Kbeta assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  33nMAssay Description:Inhibition of p110betaMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  75nMAssay Description:Inhibition of p110gammaMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of p110deltaMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  48nMAssay Description:Binding constant for PIK3CG kinase domainMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  5nMAssay Description:Binding constant for PIK3CD kinase domainMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  16nMAssay Description:Binding constant for PIK3CB kinase domainMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  66nMAssay Description:Inhibition of PI3Kgamma using PIP3 as substrate after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant PI3Kdelta assessed as inhibition of PIP3 production for 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Binding affinity to PI3Kdelta after 30 mins by competitive fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  298nMAssay Description:Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  17nMAssay Description:Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presenc...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of PI3KdeltaMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  46nMAssay Description:Inhibition of recombinant human His-tagged PI3K p110gamma expressed in baculovirus using PIP2 as substrate after 1 hr by kinase-glo luminescence assa...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  7.70nMAssay Description:In vitro renin inhibition was measured at pH 7.4 by using human plasma renin assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  2.10nMAssay Description:Binding affinity to human PI3Kbeta (P118 to S1070 residues) expressed in mammalian expression system by Kinomescan assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKd:  3.30nMAssay Description:Binding affinity to human PI3Kdelta (R108 to Q1044 residues) expressed in mammalian expression system by Kinomescan assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of recombinant full length human N-terminal His6-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf21 cells using PIP2 as...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  33nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate after 1 hr by kinase-glo luminescence assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  251nMAssay Description:Inhibition of PI3Kgamma (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  13nMAssay Description:Inhibition of PI3Kdelta (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  251nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in pre...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  54nMAssay Description:Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110beta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells ...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  39nMAssay Description:Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110delta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  181nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in pr...More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  111nMAssay Description:Inhibition of PI3Kgamma (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  16nMAssay Description:Inhibition of PI3Kdelta (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  580nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  3nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  75nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  50nMAssay Description:Inhibition of PI3Kdelta (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  251nMAssay Description:Inhibition of PI3Kbeta (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  13nMAssay Description:Inhibition of PI3Kgamma (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  13nMAssay Description:Inhibition of PI3Kgamma (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
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  251nMAssay Description:Inhibition of PI3Kbeta (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