Proteins > Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
A phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48736]
Synonyms
PI3-kinase subunit gamma;
PI3K-gamma;
PI3Kgamma;
PtdIns-3-kinase subunit gamma;
EC 2.7.1.137;
EC 2.7.1.153;
EC 2.7.1.154;
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma;
PtdIns-3-kinase subu
Research
Bioassay Publications (160)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 16 (10.00) | 29.6817 |
| 2010's | 115 (71.88) | 24.3611 |
| 2020's | 29 (18.13) | 2.80 |
Compounds (131)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| theophylline | Homo sapiens (human) | IC50 | 2,904.0000 | 1 | 1 |
| caffeine | Homo sapiens (human) | IC50 | 3,630.0000 | 1 | 1 |
| cgs 15943 | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 2.8017 | 21 | 30 |
| staurosporine | Homo sapiens (human) | IC50 | 9.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| wortmannin | Homo sapiens (human) | IC50 | 14,705.5394 | 7 | 10 |
| dasatinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| ku 55933 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 8.7950 | 2 | 2 |
| myricetin | Homo sapiens (human) | IC50 | 3.2600 | 2 | 2 |
| as 605240 | Homo sapiens (human) | IC50 | 0.0947 | 4 | 7 |
| su 11248 | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| panobinostat | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | IC50 | 0.0690 | 14 | 17 |
| PI3-Kinase alpha Inhibitor 2 | Homo sapiens (human) | IC50 | 0.1813 | 2 | 5 |
| tgx 221 | Homo sapiens (human) | IC50 | 7.7500 | 4 | 4 |
| ic 87114 | Homo sapiens (human) | IC50 | 64.0000 | 3 | 3 |
| pik 75 | Homo sapiens (human) | IC50 | 0.2476 | 1 | 4 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | IC50 | 0.5802 | 4 | 10 |
| nu 7441 | Homo sapiens (human) | IC50 | 0.2200 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| 5-(2,2-difluorobenzo(1,3)dioxol-5-ylmethylene)thiazolidine-2,4-dione | Homo sapiens (human) | IC50 | 0.2500 | 2 | 2 |
| idelalisib | Homo sapiens (human) | IC50 | 0.2781 | 29 | 29 |
| as 252424 | Homo sapiens (human) | IC50 | 0.0310 | 3 | 3 |
| liphagal | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| zstk474 | Homo sapiens (human) | GI50 | 0.0280 | 1 | 0 |
| zstk474 | Homo sapiens (human) | IC50 | 0.0369 | 11 | 10 |
| ku-0060648 | Homo sapiens (human) | IC50 | 0.5900 | 1 | 1 |
| dactolisib | Homo sapiens (human) | IC50 | 0.1022 | 20 | 20 |
| bgt226 | Homo sapiens (human) | IC50 | 0.0380 | 1 | 1 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | IC50 | 0.0260 | 2 | 2 |
| buparlisib | Homo sapiens (human) | IC50 | 0.5654 | 7 | 7 |
| ku 0063794 | Homo sapiens (human) | IC50 | 30.0000 | 2 | 2 |
| gdc 0941 | Homo sapiens (human) | IC50 | 0.6098 | 15 | 21 |
| gdc 0941 | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
| PP121 | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| gsk 2126458 | Homo sapiens (human) | IC50 | 0.0007 | 5 | 4 |
| gsk 2126458 | Homo sapiens (human) | Ki | 0.0003 | 2 | 1 |
| gne 477 | Homo sapiens (human) | IC50 | 0.0150 | 2 | 2 |
| gdc 0980 | Homo sapiens (human) | IC50 | 0.0250 | 2 | 2 |
| kin-193 | Homo sapiens (human) | IC50 | 0.9800 | 2 | 2 |
| pki 402 | Homo sapiens (human) | IC50 | 0.0114 | 3 | 3 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 6.3150 | 1 | 1 |
| pki 587 | Homo sapiens (human) | IC50 | 0.0160 | 4 | 4 |
| cp 466722 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | IC50 | 0.1500 | 2 | 1 |
| gsk 2334470 | Homo sapiens (human) | IC50 | 25.1180 | 1 | 1 |
| vs-5584 | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| etp-46321 | Homo sapiens (human) | Ki | 0.1790 | 3 | 3 |
| gsk2292767 | Homo sapiens (human) | IC50 | 0.4547 | 3 | 4 |
| gsk2292767 | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
| gsk2269557 | Homo sapiens (human) | IC50 | 6.3096 | 1 | 1 |
| ch 5132799 | Homo sapiens (human) | IC50 | 0.0360 | 2 | 1 |
| torin 1 | Homo sapiens (human) | IC50 | 0.1710 | 1 | 1 |
| ipi-145 | Homo sapiens (human) | IC50 | 0.0232 | 9 | 8 |
| gdc-0032 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 0 |
| gdc-0032 | Homo sapiens (human) | Ki | 0.0010 | 2 | 1 |
| pf-4989216 | Homo sapiens (human) | IC50 | 0.0600 | 1 | 1 |
| torin 2 | Homo sapiens (human) | IC50 | 0.0057 | 1 | 1 |
| azd8186 | Homo sapiens (human) | IC50 | 3.3375 | 2 | 2 |
| hs-173 | Homo sapiens (human) | IC50 | 0.1040 | 1 | 1 |
| cudc-907 | Homo sapiens (human) | IC50 | 0.2090 | 4 | 4 |
| lfm a13 | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
| sar245408 | Homo sapiens (human) | IC50 | 0.1473 | 3 | 2 |
| byl719 | Homo sapiens (human) | IC50 | 0.1966 | 5 | 5 |
| amg 511 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| amg319 | Homo sapiens (human) | IC50 | 0.8500 | 1 | 1 |
| sar405 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bay 80-6946 | Homo sapiens (human) | IC50 | 0.0038 | 4 | 4 |
| pp242 | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3Kα inhibitors.Bioorganic & medicinal chemistry, , 06-01, Volume: 27, Issue:11, 2019
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
(E)-1,3-diphenyl-1H-pyrazole derivatives containing O-benzyl oxime moiety as potential immunosuppressive agents: Design, synthesis, molecular docking and biological evaluation.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Kα.Bioorganic & medicinal chemistry, , Mar-15, Volume: 23, Issue:6, 2015
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.Proceedings of the National Academy of Sciences of the United States of America, , Dec-26, Volume: 103, Issue:52, 2006
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.Molecular cell, , Volume: 6, Issue:4, 2000
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.Molecular cell, , Volume: 6, Issue:4, 2000
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.Journal of medicinal chemistry, , 12-13, Volume: 61, Issue:23, 2018
Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.Proceedings of the National Academy of Sciences of the United States of America, , Dec-26, Volume: 103, Issue:52, 2006
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.Molecular cell, , Volume: 6, Issue:4, 2000
Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.Molecular cell, , Volume: 6, Issue:4, 2000
Targeting the immunity protein kinases for immuno-oncology.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.Chemistry & biology, , Feb-26, Volume: 17, Issue:2, 2010
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 48, 2021
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines.European journal of medicinal chemistry, , Volume: 57, 2012
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 28, Issue:6, 2018
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.Nature chemical biology, , Volume: 6, Issue:2, 2010
Targeting the immunity protein kinases for immuno-oncology.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.Proceedings of the National Academy of Sciences of the United States of America, , Dec-26, Volume: 103, Issue:52, 2006
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.Bioorganic & medicinal chemistry, , 11-01, Volume: 73, 2022
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
[no title available]Bioorganic & medicinal chemistry, , 09-01, Volume: 45, 2021
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
[no title available]Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 29, Issue:11, 2019
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.MedChemComm, , Mar-01, Volume: 10, Issue:3, 2019
Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Targeting the immunity protein kinases for immuno-oncology.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
[no title available]European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Identification of highly potent and selective PI3Kδ inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 27, Issue:13, 2017
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
[no title available]ACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 25, Issue:5, 2015
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Fragment based discovery of a novel and selective PI3 kinase inhibitor.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
1,3,5-Triazines: A promising scaffold for anticancer drugs development.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).ACS medicinal chemistry letters, , Aug-10, Volume: 8, Issue:8, 2017
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
L-Aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target non-conserved Asp862 of PI3KβACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 2013
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.Nature chemical biology, , Volume: 6, Issue:2, 2010
[no title available],
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 29, Issue:11, 2019
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.ACS medicinal chemistry letters, , Aug-11, Volume: 7, Issue:8, 2016
Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Recent results in protein kinase inhibition for tropical diseases.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
[no title available]Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
[no title available]ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 30, Issue:12, 2020
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) InhibJournal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo.European journal of medicinal chemistry, , Volume: 96, 2015
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.Nature chemical biology, , Volume: 6, Issue:2, 2010
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
[no title available],
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
[no title available],
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-RSC medicinal chemistry, , Oct-01, Volume: 11, Issue:10, 2020
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available],
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Identification of novel PI3K inhibitors through a scaffold hopping strategy.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.Journal of medicinal chemistry, , 12-27, Volume: 61, Issue:24, 2018
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Targeting the immunity protein kinases for immuno-oncology.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
[no title available]ACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
[no title available],
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust iJournal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
[no title available],
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
[no title available],
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3Kα inhibitors via docking-based virtual screening.Bioorganic & medicinal chemistry, , 01-01, Volume: 29, 2021
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity.European journal of medicinal chemistry, , Jul-01, Volume: 197, 2020
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| 1-phosphatidylinositol-3-kinase activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol + ATP = a 1-phosphatidyl-1D-myo-inositol 3-phosphate + ADP + 2 H+. [EC:2.7.1.137, RHEA:12709] |
| 1-phosphatidylinositol-4-phosphate 3-kinase activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4-phosphate + ATP = 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate + ADP + 2 H+. [EC:2.7.1.154, RHEA:18373] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| ephrin receptor binding | molecular function | Binding to an ephrin receptor. [GOC:ai] |
| 1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + ATP = a 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate + ADP + 2 H+. [EC:2.7.1.153, RHEA:21292] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| phosphatidylinositol 3-kinase complex, class IA | cellular component | A class I phosphatidylinositol 3-kinase complex that possesses 1-phosphatidylinositol-4-phosphate 3-kinase activity; comprises a catalytic class IA phosphoinositide 3-kinase (PI3K) subunit and an associated SH2 domain-containing regulatory subunit that is a member of a family of related proteins often called p85 proteins. Through the interaction with the SH2-containing adaptor subunits, Class IA PI3K catalytic subunits are linked to tyrosine kinase signaling pathways. [PMID:9255069, PMID:9759495] |
| phosphatidylinositol 3-kinase complex, class IB | cellular component | A class I phosphatidylinositol 3-kinase complex that possesses 1-phosphatidylinositol-4-phosphate 3-kinase activity; comprises a catalytic class IB phosphoinositide 3-kinase (PI3K) subunit and an associated regulatory subunit that is larger than, and unrelated to, the p85 proteins present in class IA complexes. Class IB PI3Ks are stimulated by G-proteins and do not interact with the SH2-domain containing adaptors that bind to Class IA PI3Ks. [PMID:9255069, PMID:9759495] |
Involved In
This protein is involved in 40 target(s):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
| adaptive immune response | biological process | An immune response mediated by cells expressing specific receptors for antigens produced through a somatic diversification process, and allowing for an enhanced secondary response to subsequent exposures to the same antigen (immunological memory). [GO_REF:0000022, GOC:add, ISBN:0781735149] |
| dendritic cell chemotaxis | biological process | The movement of a dendritic cell in response to an external stimulus. [CL:0000451, GOC:add, ISBN:0781735149, PMID:15814331, PMID:16056255] |
| positive regulation of acute inflammatory response | biological process | Any process that activates or increases the frequency, rate, or extent of an acute inflammatory response. [GOC:add] |
| respiratory burst involved in defense response | biological process | A phase of elevated metabolic activity, during which oxygen consumption increases made as part of a defense response ; this leads to the production, by an NADH dependent system, of hydrogen peroxide (H2O2), superoxide anions and hydroxyl radicals. [GOC:add, ISBN:0781735149, PMID:12789499] |
| sphingosine-1-phosphate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by sphingosine-1-phosphate binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ascb_2009, GOC:signaling, PMID:14592418, PMID:22001186, Reactome:R-HSA-419428] |
| endocytosis | biological process | A vesicle-mediated transport process in which cells take up external materials or membrane constituents by the invagination of a part of the plasma membrane to form a new membrane-bounded vesicle. [GOC:mah, ISBN:0198506732, ISBN:0716731363, Wikipedia:Endocytosis] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| positive regulation of endothelial cell migration | biological process | Any process that increases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb] |
| T cell chemotaxis | biological process | The directed movement of a T cell in response to an external stimulus. A T cell is a type of lymphocyte whose defining characteristic is the expression of a T cell receptor complex. [GOC:dph, GOC:tb] |
| negative regulation of triglyceride catabolic process | biological process | Any process that decreases the frequency, rate, or extent of the chemical reactions and pathways resulting in the breakdown of triglyceride. [GOC:rn, GOC:tb] |
| neutrophil chemotaxis | biological process | The directed movement of a neutrophil cell, the most numerous polymorphonuclear leukocyte found in the blood, in response to an external stimulus, usually an infection or wounding. [GOC:jl, ISBN:0198506732] |
| secretory granule localization | biological process | Any process in which a secretory granule is transported to, and/or maintained in, a specific location within the cell. [GOC:mah] |
| regulation of cell adhesion mediated by integrin | biological process | Any process that modulates the frequency, rate, or extent of cell adhesion mediated by integrin. [GOC:add] |
| positive regulation of Rac protein signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of Rac protein signal transduction. [GOC:bf] |
| natural killer cell chemotaxis | biological process | The directed movement of a natural killer cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [CL:0000623, GOC:BHF] |
| T cell proliferation | biological process | The expansion of a T cell population by cell division. Follows T cell activation. [GOC:jl] |
| T cell activation | biological process | The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| mast cell degranulation | biological process | The regulated exocytosis of secretory granules containing preformed mediators such as histamine, serotonin, and neutral proteases by a mast cell. [ISBN:0781735149] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
| innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
| regulation of angiogenesis | biological process | Any process that modulates the frequency, rate or extent of angiogenesis. [GOC:go_curators] |
| phosphatidylinositol phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol phosphate. [ISBN:0198506732] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| negative regulation of cardiac muscle contraction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cardiac muscle contraction. [GOC:ecd] |
| platelet aggregation | biological process | The adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:BHF, GOC:vk] |
| cellular response to cAMP | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:mah] |
| neutrophil extravasation | biological process | The migration of a neutrophil from the blood vessels into the surrounding tissue. [CL:0000775, GOC:BHF] |
| hepatocyte apoptotic process | biological process | Any apoptotic process in a hepatocyte, the main structural component of the liver. [CL:0000182, GOC:jc, GOC:mtg_apoptosis, PMID:15856020] |
| regulation of calcium ion transmembrane transport | biological process | Any process that modulates the frequency, rate or extent of calcium ion transmembrane transport. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:24125847] |
| negative regulation of fibroblast apoptotic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of fibroblast apoptotic process. [GOC:mtg_apoptosis, GOC:obol, GOC:yaf] |
| cell migration | biological process | The controlled self-propelled movement of a cell from one site to a destination guided by molecular cues. [GOC:cjm, GOC:dph, GOC:ems, GOC:pf, Wikipedia:Cell_migration] |
| phosphatidylinositol-mediated signaling | biological process | The series of molecular signals in which a cell uses a phosphatidylinositol-mediated signaling to convert a signal into a response. Phosphatidylinositols include phosphatidylinositol (PtdIns) and its phosphorylated derivatives. [GOC:bf, GOC:ceb, ISBN:0198506732] |
| phosphatidylinositol-3-phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol-3-phosphate, a phosphatidylinositol monophosphate carrying the phosphate group at the 3-position. [GOC:al, GOC:vw] |