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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 562 hits for monomerid = 25028
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataKi: 1.40nMAssay Description:Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataKi: 1.54nMAssay 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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 1.54nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 2.56nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 2.56nMAssay 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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 2.60nMAssay Description:Inhibition of GST-fused human recombinant PI3Kalpha expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 31nMAssay Description:Inhibition of GST-fused human recombinant PI3Kdelta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKi: 41.8nMAssay 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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataKi: 41.8nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
Affinity DataKi: 70.2nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
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
Affinity DataKi: 570nMAssay Description:Inhibition of human recombinant mTOR assessed as reduction in GFP-4EBP1 phosphorylation after 30 mins by FRET assayMore data for this Ligand-Target Pair
Affinity DataKi: 580nM ΔG°: -8.50kcal/molepH: 7.5 T: 2°CAssay Description:Mammalian target of rapamycin (mTOR) was assayed by monitoring phosphorylation of GFP-4EBP using a homogeneous time-resolved fluorescence resonance e...More data for this Ligand-Target Pair
Affinity DataKi: 580nMAssay Description:Inhibition of human recombinant mTOR expressed in insect cells assessed as phosphorylation of recombinant (GFP)-4-EBP1 measured after 30 mins by fluo...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))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform [H1047R](Homo sapiens (Human))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform [E545K](Homo sapiens (Human))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...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))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 33nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...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))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataIC50: 75nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta(Homo sapiens (Human))
Piramed Pharma
Piramed Pharma
Affinity DataIC50: 670nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for ABL1(F317L)-phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PRKD2 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L858R) kinase domainMore data for this Ligand-Target Pair
TargetCalcium/calmodulin-dependent protein kinase type II subunit alpha(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CAMK2A kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(E746-A750del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for SRPK2 kinase domainMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for FLT4 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L861Q) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MYO3B kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MET(Y1235D) kinase domainMore data for this Ligand-Target Pair
TargetInhibitor of nuclear factor kappa-B kinase subunit alpha(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for IKK-alpha kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PRKCH kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CDK4-cyclinD1 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domainMore data for this Ligand-Target Pair
TargetCalcium/calmodulin-dependent protein kinase type II subunit beta(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CAMK2B kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EPHA6 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(G719C) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CDC2L2 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CHEK1 kinase domainMore data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: 710nMAssay Description:Binding constant for FLT3(D835Y) kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase MRCK gamma(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DMPK2 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MET kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for FGFR3(G697C) kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase TNNI3K(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for TNNI3K kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for ABL1-phosphorylated kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataKd: 4.5nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for LRRK2(G2019S) kinase domainMore data for this Ligand-Target Pair