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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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 99 hits for monomerid = 25028   

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
In DepthDetails ArticlePubMed
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
In DepthDetails ArticlePubMed
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
In DepthDetails ArticlePubMed
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:  670nMpH: 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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Homo sapiens (Human))
Piramed Pharma

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.00E+4nMpH: 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
In DepthDetails ArticlePubMed
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 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:  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:  590nMAssay Description:Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of human PI3KC2alpha by non-radiometric ADP-Glo assayMore 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 human PI3KCdelta by non-radiometric ADP-Glo assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  410nMAssay Description:Inhibition of human mTOR by non-radiometric ADP-Glo 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
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  580nMAssay Description:Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide substrate incubated for 1 hr by TR-FRET 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 PI substrate incubated for 60 mins by kinase-glo luminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  580nMAssay Description:Inhibition of mTOR (unknown origin) using ULight4E-BP1 peptide as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  310nMAssay Description:Inhibition of human recombinant mTOR by FRETMore 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 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:  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 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 p110alphaMore 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 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 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:  66nMAssay Description:Inhibition of PI3Kgamma using PIP3 as substrate after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Spanish National Cancer Research Centre (Cnio)

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  6.40E+4nMAssay Description:Displacement of [3H]-astemizole from human ERG expressed in CHO-K1 cells membraneMore 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 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
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PI3KC2alpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  410nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  590nMAssay 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))
Piramed Pharma

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of Vps34 (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 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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:  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:  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
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  1.52E+4nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  2.70E+3nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed