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.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 25028   

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:  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 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:  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 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 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 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:  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:  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:  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:  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:  324nMAssay Description:Inhibition of human PI3K p110beta by HTRF assayMore data for this Ligand-Target Pair
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  31nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)
Affinity DataIC50:  146nMAssay Description:Inhibition of PI3Kbeta 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