Found 20 hits Enz. Inhib. hit(s) with Target = 'Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform' and Ligand = 'BDBM12915' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 940 | n/a | n/a | n/a | n/a | n/a | n/a |
School of Traditional Chinese Pharmacy
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs by fluorescence polarization assay |
Bioorg Med Chem 27: 2261-2267 (2019)
Article DOI: 10.1016/j.bmc.2019.04.021 BindingDB Entry DOI: 10.7270/Q2MC93B4 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 947 | n/a | n/a | n/a | n/a | n/a | n/a |
Nanjing University
Curated by ChEMBL
| Assay Description Inhibition of recombinant PI3Kgamma (unknown origin) using PI(3,4)P2 as substrate after 3 hrs incubation by competitive fluorescence polarization kin... |
Bioorg Med Chem 23: 1231-40 (2015)
Article DOI: 10.1016/j.bmc.2015.01.052 BindingDB Entry DOI: 10.7270/Q2BC417K |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 950 | n/a | n/a | n/a | n/a | n/a | n/a |
School of Traditional Chinese Pharmacy
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay |
Eur J Med Chem 182: (2019)
Article DOI: 10.1016/j.ejmech.2019.111630 BindingDB Entry DOI: 10.7270/Q2W380Q5 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB US Patent
| n/a | n/a | 1.06E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
SignalRx Pharmaceuticals, Inc.
US Patent
| Assay Description Several TP Scaffold compounds were tested for inhibition activity against isoforms of PI3K (alpha, beta, gamma, and delta isoforms) and the bromodoma... |
US Patent US9505780 (2016)
BindingDB Entry DOI: 10.7270/Q22B8WZ1 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB US Patent
| n/a | n/a | 1.06E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai... |
J Med Chem 50: 2647-54 (2007)
BindingDB Entry DOI: 10.7270/Q24170D7 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Cincinnati
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma by luminescent kinase glo assay |
Bioorg Med Chem Lett 19: 2215-9 (2009)
Article DOI: 10.1016/j.bmcl.2009.02.115 BindingDB Entry DOI: 10.7270/Q2KP833D |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.40E+3 | 210 | n/a | n/a | n/a | 7.2 | 20 |
MRC
| Assay Description Binding was detected as a change in the intrinsic tryptophan fluorescence of the PI3K upon the addition of inhibitor. The inhibitor was incubated wit... |
Mol Cell 6: 909-19 (2000)
Article DOI: 10.1016/s1097-2765(05)00089-4 BindingDB Entry DOI: 10.7270/Q22F7KPC |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.50E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
La Trobe University
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma (unknown origin) incubated for 60 mins by kinase-glo luminescence assay |
Eur J Med Chem 110: 326-39 (2016)
Article DOI: 10.1016/j.ejmech.2016.01.042 BindingDB Entry DOI: 10.7270/Q2H133V6 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.60E+3 | n/a | n/a | n/a | n/a | 7.4 | 22 |
Astellas Pharma Inc.
| Assay Description The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft... |
Bioorg Med Chem 15: 403-12 (2007)
Article DOI: 10.1016/j.bmc.2006.09.047 BindingDB Entry DOI: 10.7270/Q2SJ1HXZ |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.60E+3 | n/a | n/a | n/a | n/a | 7.4 | 22 |
Astellas Pharma Inc.
| Assay Description The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft... |
Bioorg Med Chem 15: 5837-44 (2007)
Article DOI: 10.1016/j.bmc.2007.05.070 BindingDB Entry DOI: 10.7270/Q2X928M7 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Astellas Pharma Inc.
Curated by ChEMBL
| Assay Description Inhibition of p110gamma |
Bioorg Med Chem Lett 17: 2438-42 (2007)
Article DOI: 10.1016/j.bmcl.2007.02.032 BindingDB Entry DOI: 10.7270/Q28053F2 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.78E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Arizona
Curated by ChEMBL
| Assay Description Inhibition of PI3K p110gamma (unknown origin) |
J Med Chem 56: 1922-39 (2013)
Article DOI: 10.1021/jm301522m BindingDB Entry DOI: 10.7270/Q2Z89DR9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 3.02E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Newcastle University
Curated by ChEMBL
| Assay Description Inhibition of PI-3K gamma (unknown origin) |
J Med Chem 56: 6386-401 (2013)
Article DOI: 10.1021/jm400915j BindingDB Entry DOI: 10.7270/Q2RF5WFD |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 6.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma using phosphatidylinositol as substrate by gamma33P[ATP] incorporation assay |
J Med Chem 55: 8559-81 (2012)
Article DOI: 10.1021/jm300847w BindingDB Entry DOI: 10.7270/Q2SN0B47 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 7.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Anhui Agricultural University
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma (unknown origin) after 4 hrs |
Eur J Med Chem 108: 586-93 (2016)
Article DOI: 10.1016/j.ejmech.2015.12.020 BindingDB Entry DOI: 10.7270/Q2T72K8V |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 7.26E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Jordan
Curated by ChEMBL
| Assay Description Inhibition of PI3Kgamma (unknown origin) assessed as decrease in fluorescence intensity using phosphorylated substrate |
Eur J Med Chem 84: 454-65 (2014)
Article DOI: 10.1016/j.ejmech.2014.07.056 BindingDB Entry DOI: 10.7270/Q2057HM8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article
| n/a | n/a | 7.26E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Inhibition of PI3Kgamma (unknown origin) using [33gammaP]ATP and phosphotidylinositol as substrate by scintillation proximity assay |
Citation and Details
Article DOI: 10.1007/s00044-013-0561-0 BindingDB Entry DOI: 10.7270/Q2TT4TV0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 7.26E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Serono Pharmaceutical Research Institute
Curated by ChEMBL
| Assay Description Inhibition of human PI3Kgamma |
J Med Chem 49: 3857-71 (2006)
Article DOI: 10.1021/jm0601598 BindingDB Entry DOI: 10.7270/Q2DZ07X0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 7.30E+3 | n/a | n/a | n/a | n/a | 7.4 | 22 |
TargeGen Inc.
| Assay Description The luminescence-based kinase assay with recombinant phosphatidylinositol 3-kinase (Upstate Cell Signaling Solutions) was used for the determination ... |
Proc Natl Acad Sci U S A 103: 19866-71 (2006)
Article DOI: 10.1073/pnas.0606956103 BindingDB Entry DOI: 10.7270/Q2J101GM |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
(Homo sapiens (Human)) | BDBM12915
(2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |...)Show InChI InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2 | PDB MMDB
NCI pathway Reactome pathway KEGG
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| DrugBank PDB Article PubMed
| n/a | n/a | 1.20E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University Hospital Hradec Kralove
Curated by ChEMBL
| Assay Description Inhibition of PI3K p110gamma (unknown origin) |
J Med Chem 58: 41-71 (2015)
Article DOI: 10.1021/jm501026z BindingDB Entry DOI: 10.7270/Q2P84DJ7 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |