BDBM50274649 CHEMBL4129600::US10858355, Example 30

SMILES CNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C

InChI Key InChIKey=LHKIAELCKQHVBI-NSHDSACASA-N

Data  15 IC50

  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 15 hits for monomerid = 50274649   

TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  398nMAssay Description:Inhibition of PI3Kdelta in human JeKo1B cells assessed as reduction in AKT phosphorylation at ser473 residue preincubated for 60 mins followed by ant...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  398nMAssay Description:Inhibition of PI3Kdelta in anti-IgM-stimulated human JeKo-1 cells assessed as inhibition of AKT phosphorylation at Ser473 residue incubated for 60 mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  0.794nMAssay Description:Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  2.51E+4nMAssay Description:Inhibition of recombinant human 6His-tagged PI3K p110beta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate additi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  158nMAssay Description:Inhibition of recombinant human 6His-tagged PI3K p110delta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  3.98E+3nMAssay Description:Inhibition of recombinant human 6His-tagged PI3K p110alpha/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Mus musculus (Mouse))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kgamma in mouse RAW264 cells assessed as reduction in Akt phosphorylation at Ser473 residue preincubated for 15 mins followed by C5a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50: <3.16E+4nMAssay Description:Inhibition of PI3Kbeta in human MDA-MB-468 cells assessed as reduction in Akt phosphorylation at Tyr308 residue after 2 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50: <3.16E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  0.794nMAssay Description:The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  1.26nMAssay Description:The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  0.794nMAssay Description:Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  158nMAssay Description:Inhibition of recombinant human PI3Kdelta assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Mus musculus (Mouse))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kgamma in C5a-stimulated mouse RAW 264 cells assessed as inhibition of AKT phosphorylation at Ser473 residue Pretreated for 15 mins ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50274649(CHEMBL4129600 | US10858355, Example 30)
Affinity DataIC50: <3.16E+4nMAssay Description:Inhibition of PI3Kalpha in human BT474 cells assessed as reduction in Akt phosphorylation at Tyr308 residue after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed