BDBM368657 US10227350, Compound 105::US10227350, Compound 106::US10227350, Compound 75

SMILES Cc1nc2c(cc(cc2n1-c1ccnc2c(F)ccc(F)c12)-c1ccnc(N)c1F)-c1nnc[nH]1

InChI Key InChIKey=SBVBUGSOYHJGGD-UHFFFAOYSA-N

Data  28 IC50  5 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 33 hits for monomerid = 368657   

TargetPhosphatidylinositol 3-kinase regulatory subunit beta(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  3nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 3-kinase regulatory subunit beta(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  3nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails US Patent
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  188nMAssay Description:Inhibition of full length human p110alpha/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  188nMAssay Description:Inhibition of full length human p110alpha/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  1.42E+3nMAssay Description:Inhibition of full length human His-tagged p110beta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of full length human p110delta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  42nMAssay Description:Inhibition of full length human p110delta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of full length human PI3Kgamma using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  4.16E+3nMAssay Description:Inhibition of full length human PI3Kgamma using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of full length human p110alpha/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  2nMAssay Description:Inhibition of full length human His-tagged p110beta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  43nMAssay Description:Inhibition of full length human p110delta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  4.27E+3nMAssay Description:Inhibition of full length human PI3Kgamma using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  1.42E+3nMAssay Description:Inhibition of full length human His-tagged p110beta/p85alpha using PIP2 as substrate after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  3nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  3nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  2nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  262nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  262nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  43nMAssay 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
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  42nMAssay 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
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >1.00E+4nMAssay 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
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  4.16E+3nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of human CYP3A4More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataEC50:  9nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataEC50:  15nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataEC50:  53nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataEC50:  12nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataEC50:  6nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetCytochrome P450 4B1(Homo sapiens)
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of human CYP450More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 3-kinase regulatory subunit beta(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM368657(US10227350, Compound 105 | US10227350, Compound 10...)
Affinity DataIC50:  1.40E+3nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails US Patent