Compile Data Set for Download or QSAR
Report error Found 11981 Enz. Inhib. hit(s) with Target = 'Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform'
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
LigandPNGBDBM27817(2-{[2-({1-[2-(dimethylamino)acetyl]-5-methoxy-2,3-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM482158(TAE684 | BDBM50242742)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM60665(US9145414, R406 | US9212178, R406 | BDBM50249542)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50184807((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-me...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM36409(CID24905147 | 2-(4-amino-1-isopropyl-1H-pyrazolo[3...)
Affinity DataKd:  200nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50336878(2-morpholino-N6-(tetrahydro-2H-pyran-4-yl)-4,5'-bi...)
Affinity DataEC50:  220nMAssay Description:Inhibition of PI3Kalpha-mediated Akt phosphorylation at Ser473 in human A2780 cells after 1 hrMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM31085(cid_11409972 | 1-[4-[(4-ethylpiperazin-1-yl)methyl...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355499(CHEMBL1908395 | CHEMBL1908842)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50140272(CHEMBL3754572)
Affinity DataEC50: <40nMAssay Description:Inhibition of PI3Kalpha in human A2780 cells assessed as reduction of AKT phosphorylation at Ser473 after 1 hrMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/5/2017
Entry Details Article
PubMed
LigandPNGBDBM16673(Xarelto | BAY439006 | CHEMBL1336 | BAY 43-9006 | 4...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50200977(CHEMBL3986383 | US10087187, Compound 5)
Affinity DataKd:  617nMAssay Description:Binding affinity to human PI3Kalpha (108 to 1068 residues) expressed in mammalian expression system by KINOMEscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/31/2018
Entry Details Article
PubMed
LigandPNGBDBM21(VANDETANIB | N-(4-bromo-2-fluorophenyl)-6-methoxy-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
LigandPNGBDBM26300(cid_16007391 | 2-{3-[(7-{3-[ethyl(2-hydroxyethyl)a...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
LigandPNGBDBM50602331(CHEMBL5182371)
Affinity DataEC50:  52nMAssay Description:Inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation after 24 hrs by electrochemiluminescent ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM13336(4-{4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355499(CHEMBL1908395 | CHEMBL1908842)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM4552(CHEMBL288441 | SKI-606 | 4-[(2,4-Dichloro-5-methox...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50184807((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-me...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355504(CHEMBL1908393)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355496(CHEMBL1908397)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM12621(2,4-Diamino-5-ketopyrimidine 39 | 5-[(2,3-difluoro...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E545K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355504(CHEMBL1908393)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
LigandPNGBDBM50184807((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-me...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355494(CHEMBL1908396)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM31095(5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-yli...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25118(4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM21(VANDETANIB | N-(4-bromo-2-fluorophenyl)-6-methoxy-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355495(CHEMBL1908391)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50467459(CHEMBL4284892)
Affinity DataEC50:  8.90E+3nMAssay Description:Inhibition of PI3Kalpha H1047R mutant (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM36409(CID24905147 | 2-(4-amino-1-isopropyl-1H-pyrazolo[3...)
Affinity DataKd:  190nMAssay Description:Binding constant for PIK3CA(E545K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM15244(cid_3038525 | 5-(2,6-dichlorophenyl)-2-[(2,4-diflu...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM13530(cid_5291 | STI571 | N-(4-methyl-3-{[4-(pyridin-3-y...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50128285(3-(1-Methyl-1H-indol-3-yl)-4-[1-(1-pyridin-2-ylmet...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM16673(Xarelto | BAY439006 | CHEMBL1336 | BAY 43-9006 | 4...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM24773(N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyr...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50300690(CHEMBL576982 | N-(5-tert-Butyl-isoxazol-3-yl)-N'-{...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to PIK3CAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
LigandPNGBDBM50341216(9-(6-aminopyridin-3-yl)-1-(3-chloro-4-fluorophenyl...)
Affinity DataEC50:  250nMAssay Description:Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblottingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
LigandPNGBDBM50467465(CHEMBL4292792)
Affinity DataEC50:  6.30E+3nMAssay Description:Inhibition of PI3Kalpha H1047R mutant (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM50315213(TCMDC-137004 | 2-(difluoromethyl)-1-(4,6-dimorphol...)
Affinity DataEC50:  50nMAssay Description:Inhibition of PI3Kalpha H1047R mutant (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50161957(CHEMBL180022 | N-(4-(3-chloro-4-(pyridin-2-ylmetho...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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