null
SMILES Cc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1ccnc(c1)C(C)(C)C(F)(F)F
InChI Key InChIKey=STUWGJZDJHPWGZ-LBPRGKRZSA-N
PDB links: 8 PDB IDs match this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 45 hits for monomerid = 50436459
TargetCytochrome P450 3A4(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
3D Structure (crystal)TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 5nMAssay Description:Inhibition of P110alpha (unknown origin) using L-a-phosphatidylinositol as substrate by luminescence assayMore data for this Ligand-Target Pair
TargetCellular tumor antigen p53(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of p53 (unknown origin) phosphorylation at Ser15 by cell-based assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of N-terminal myristoylated P110delta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISAMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of N-terminal myristoylated P110beta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISAMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 74nMAssay Description:Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISAMore data for this Ligand-Target Pair
TargetDNA-dependent protein kinase catalytic subunit(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of DNA-PK (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of myristoylated human P110beta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analys...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of myristoylated human P110delta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analy...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 290nMAssay Description:Inhibition of P110delta (unknown origin) using PI or PIP2:PS as substrate measured for 15 to 60 mins by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 250nMAssay Description:Inhibition of P110gamma (unknown origin) using PI or PIP2:PS as substrate measured for 15 to 60 mins by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of P110beta (unknown origin) by Kinase-Glo assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 5nMAssay Description:Inhibition of P110alpha (unknown origin) by Kinase-Glo assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 74nMAssay Description:Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analy...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 4.60nMAssay Description:Inhibition of recombinant PI3Kalpha (unknown origin) by KinaseGlo assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 250nMAssay Description:Inhibition of P110gamma (unknown origin) using PIP2:PS as substrate by TR-FRET assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 290nMAssay Description:Inhibition of P110delta (unknown origin) using PIP2:PS as substrate by TR-FRET assayMore data for this Ligand-Target Pair
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of ATM (unknown origin) phosphorylation at Ser1981 by cell-based assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase ATR(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of ATR (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of VPS34 (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 5nMAssay Description:Inhibition of P13Kalpha (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 290nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kalpha (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
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of PI3Kbeta in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serumMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 250nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 3.90nMAssay Description:Inhibition of His-tagged human full length PI3Kalpha coexpressed with p85 alpha in baculovirus expression system using PIP2 peptide as substrate incu...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 1.54E+3nMAssay Description:Inhibition of N-terminal His6-tagged human recombinant full length PI3Kbeta co-expressed with human recombinant full length P85alpha in baculovirus i...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 94nMAssay Description:Inhibition of GST-tagged human recombinant PI3Kgamma catalytic domain (468 to 1203 residues) expressed in insect cells using PIP2 peptide as substrat...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.46E+3nMAssay Description:Inhibition of N-terminal FLAG-tagged human recombinant mTOR (1362 to end residues) using ULight-4E-BP1 (Thr37/46) peptide as substrate incubated for ...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 72nMAssay Description:Inhibition of N-terminal His6-tagged human recombinant full length PI3Kdelta co-expressed with human recombinant full length P85alpha in baculovirus ...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 18nMAssay Description:Inhibition of human PI3Kalpha using PIP2 as substrate in presence of ATP measured after 30 mins by HTRF assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 1.84E+3nMAssay Description:Inhibition of human PI3K p110beta/p85alpha using PIP2 as substrate incubated for 40 mins in presence of ATP measured after 40 mins by HTRF assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 383nMAssay Description:Inhibition of human PI3K p110delta/p85alpha using PIP2 as substrate in presence of ATP measured after 40 mins by HTRF assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of mTOR in TSC1 null human MCF7 cells assessed as decrease in p70S6K phosphorylation at Thr389 residue incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 510nMAssay Description:Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110delta expressed in rat Rat1 cellsMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 3.40E+3nMAssay Description:Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110beta expressed in rat Rat1 cellsMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 200nMAssay Description:Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110alpha expressed in rat Rat1 cellsMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 139nMAssay Description:Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.15E+3nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 190nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))TBA
Affinity DataIC50: 9.5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of P110beta (unknown origin) using L-a-phosphatidylinositol as substrate by luminescence assayMore data for this Ligand-Target Pair