BDBM50059637 GSK-2636771::GSK2636771::US10660898, Example 31

SMILES Cc1nc2c(cc(cc2n1Cc1cccc(c1C)C(F)(F)F)N1CCOCC1)C(O)=O

InChI Key InChIKey=XTKLTGBKIDQGQL-UHFFFAOYSA-N

Data  12 IC50  5 EC50

  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 17 hits for monomerid = 50059637   

TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  0.890nMAssay Description:Inhibition of PI3K p110beta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50: >1.30E+4nMAssay Description:Inhibition of acetylcholinesterase (AChE) activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  25nMAssay Description:Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human full length p110alpha/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  300nMAssay Description:Inhibition of human p110delta catalytic subunit/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET as...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human full length p110gamma using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataEC50:  23nMAssay Description:Inhibition of PI3Kbeta in PTEN-deficient human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataEC50:  42nMAssay Description:Inhibition of PI3Kbeta in PTEN-deficient human LNCaP C4-2 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesosca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataEC50:  178nMAssay Description:Inhibition of PI3Kbeta in PTEN-deficient human LNCAP cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale as...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataEC50:  40nMAssay Description:Inhibition of PI3Kbeta in PTEN-deficient human MDA-MB-415 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesosca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataEC50:  28nMAssay Description:Inhibition of PI3Kbeta in PTEN-deficient human ZR-75-1 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  48nMAssay Description:Inhibition of PI3Kbeta in human 786-O cells assessed as reduction in phosphorylation of AKT at 473 measured after 1 hr by alpha screen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  22nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate in presence of ATP measured after 45 mins by HTRF assay relative to controlMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50: >5.80E+3nMAssay Description:Inhibition of choline acetyltransferase (ChAT) activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University Hospital Hradec Kralove

Curated by ChEMBL
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  5.20nMAssay Description:Inhibition of choline acetyltransferase (ChAT) activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  58nMAssay Description:Inhibition of choline acetyltransferase (ChAT) activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50059637(GSK-2636771 | GSK2636771 | US10660898, Example 31)
Affinity DataIC50:  6.31nMAssay Description:PI3Kinase Reaction Buffer was prepared by diluting the stock 1:4 with de-ionized water. Freshly prepared DTT was added at a final concentration of 5 ...More data for this Ligand-Target Pair
In DepthDetails US Patent