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::US12054488, Compound GDC0941

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

InChI Key InChIKey=LHNIIDJUOCFXAP-UHFFFAOYSA-N

Data  14 KI  100 IC50  450 Kd  1 EC50

  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 581 hits for monomerid = 25028   

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 0.00300nMAssay Description:Inhibition of p110 alpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 0.00300nMAssay Description:Inhibition of p110 delta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 0.0330nMAssay Description:Inhibition of p110 beta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 0.0750nMAssay Description:Inhibition of p110 gamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
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 Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
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 Depth
Date in BDB:
10/8/2019
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
4/12/2014
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
3/4/2019
Entry Details
US Patent

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
In Depth
Date in BDB:
7/12/2021
Entry Details
US Patent

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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
10/8/2019
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/12/2021
Entry Details
US Patent

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataKi:  2.56nMAssay 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 Depth
Date in BDB:
3/4/2019
Entry Details
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 Depth
Date in BDB:
4/12/2014
Entry Details Article
PubMed
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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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 Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/28/2017
Entry Details Article
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged human recombinant PI3K-p110alpha expressed in baculovirus-infected Sf9 cells incubated for 1 hr by microbeta counter analysi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
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 Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged human recombinant PI3K-p110gamma expressed in baculovirus-infected Sf9 cells incubated for 1 hr by microbeta counter analysi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged human recombinant PI3K-p110delta expressed in baculovirus-infected Sf9 cells incubated for 1 hr by microbeta counter analysi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged human recombinant PI3K-p110beta expressed in baculovirus-infected Sf9 cells incubated for 1 hr by microbeta counter analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged human recombinant PI3K-p110alpha E545A mutant expressed in baculovirus-infected Sf9 cells incubated for 1 hr by microbeta co...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Ain Shams University

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
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 Depth
Date in BDB:
3/30/2016
Entry Details Article
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 Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:TBDMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
US Patent

LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:TBDMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
US Patent

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 Depth
Date in BDB:
11/19/2010
Entry Details Article
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of p110deltaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
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 Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
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 Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
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 Depth
Date in BDB:
3/14/2016
Entry Details Article
PubMed
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 Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
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 Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3KdeltaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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 Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
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
In Depth
Date in BDB:
2/16/2020
Entry Details Article
PubMed
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
In Depth
Date in BDB:
10/8/2019
Entry Details Article
PubMed
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 Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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