Proteins > Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
A phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform that is encoded in the genome of human. [PRO:DNx, UniProtKB:P42338]
Synonyms
PI3-kinase subunit beta;
PI3K-beta;
PI3Kbeta;
PtdIns-3-kinase subunit beta;
EC 2.7.1.153;
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta;
PtdIns-3-kinase subunit p110-beta;
p110beta
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 | 13 (8.13) | 29.6817 |
| 2010's | 112 (70.00) | 24.3611 |
| 2020's | 35 (21.88) | 2.80 |
Compounds (124)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
[no title available]Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Synthetic Lethality through the Lens of Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
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
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
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
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
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
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
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
Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.Bioorganic & medicinal chemistry, , May-15, Volume: 20, Issue:10, 2012
Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
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
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
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
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
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
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
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
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
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
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
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 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
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
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
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
Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ.Bioorganic & medicinal chemistry, , 09-01, Volume: 69, 2022
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 antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
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
Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
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 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
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
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
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
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
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
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
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, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
[no title available]Bioorganic & medicinal chemistry, , 09-01, Volume: 45, 2021
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
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
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
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
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.MedChemComm, , Mar-01, Volume: 10, Issue:3, 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
[no title available]Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 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
Targeting the immunity protein kinases for immuno-oncology.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 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
[no title available]European journal of medicinal chemistry, , May-10, Volume: 151, 2018
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
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
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
Identification of highly potent and selective PI3Kδ inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 27, Issue:13, 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
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
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
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
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
Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
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],
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
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 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 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
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
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
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
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
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
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
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
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 antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
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 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
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
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
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
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
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
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
Designing multi-targeted agents: An emerging anticancer drug discovery paradigm.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
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
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
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 211, 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
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
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
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Discovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
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
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
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
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 Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.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
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],
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
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
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
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 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
Designing multi-targeted agents: An emerging anticancer drug discovery paradigm.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
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
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
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
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 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
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
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
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 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 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| insulin receptor substrate binding | molecular function | Binding to an insulin receptor substrate (IRS) protein, an adaptor protein that bind to the transphosphorylated insulin and insulin-like growth factor receptors, are themselves phosphorylated and in turn recruit SH2 domain-containing signaling molecules to form a productive signaling complex. [PMID:12829233] |
| 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] |
| 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] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| 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] |
| midbody | cellular component | A thin cytoplasmic bridge formed between daughter cells at the end of cytokinesis. The midbody forms where the contractile ring constricts, and may persist for some time before finally breaking to complete cytokinesis. [ISBN:0815316194] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
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 | cellular component | A protein complex capable of phosphatidylinositol 3-kinase activity and containing subunits of any phosphatidylinositol 3-kinase (PI3K) enzyme. These complexes are divided in three classes (called I, II and III) that differ for their presence across taxonomic groups and for the type of their constituents. Catalytic subunits of phosphatidylinositol 3-kinase enzymes are present in all 3 classes; regulatory subunits of phosphatidylinositol 3-kinase enzymes are present in classes I and III; adaptor proteins have been observed in class II complexes and may be present in other classes too. [GOC:bf, PMID:24587488] |
Involved In
This protein is involved in 30 target(s):
| Target | Category | Definition |
|---|
| endothelial cell proliferation | biological process | The multiplication or reproduction of endothelial cells, resulting in the expansion of a cell population. Endothelial cells are thin flattened cells which line the inside surfaces of body cavities, blood vessels, and lymph vessels, making up the endothelium. [GOC:add, ISBN:0781735149] |
| response to ischemia | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a inadequate blood supply. [GOC:hjd] |
| 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] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| 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] |
| autophagy | biological process | The cellular catabolic process in which cells digest cellular materials, such as organelles and other macromolecular constituents, or non-self materials such as intracellular pathogens. Autophagy serves to provide essential nutrients under conditions of cellular stress; or can remodel intracellular structures during cell differentiation. [GOC:autophagy, ISBN:0198547684, PMID:11099404, PMID:29455577, PMID:9412464] |
| chemotaxis | biological process | The directed movement of a motile cell or organism, or the directed growth of a cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [ISBN:0198506732] |
| homophilic cell adhesion via plasma membrane adhesion molecules | biological process | The attachment of a plasma membrane adhesion molecule in one cell to an identical molecule in an adjacent cell. [ISBN:0198506732] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| 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] |
| positive regulation of autophagy | biological process | Any process that activates, maintains or increases the rate of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| 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] |
| 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] |
| platelet activation | biological process | A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/] |
| positive regulation of neutrophil apoptotic process | biological process | Any process that activates or increases the frequency, rate, or extent of neutrophil apoptotic process. [GOC:add, GOC:mtg_apoptosis] |
| 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] |
| embryonic cleavage | biological process | The first few specialized divisions of an activated animal egg. [GOC:clt, ISBN:0070524300] |
| negative regulation of MAPK cascade | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of signal transduction mediated by the MAPKKK cascade. [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] |
| phosphatidylinositol phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol phosphate. [ISBN:0198506732] |
| negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| angiogenesis involved in wound healing | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels and contribute to the series of events that restore integrity to a damaged tissue, following an injury. [GOC:dph, PMID:15039218] |
| platelet aggregation | biological process | The adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:BHF, GOC:vk] |
| negative regulation of vascular endothelial growth factor signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular endothelial growth factor signaling pathway. [GOC:TermGenie] |
| negative regulation of hypoxia-induced intrinsic apoptotic signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of hypoxia-induced intrinsic apoptotic signaling pathway. [GO_REF:0000058, GOC:bf, GOC:PARL, GOC:TermGenie, PMID:24553947] |
| negative regulation of sprouting angiogenesis | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of sprouting angiogenesis. [GO_REF:0000058, GOC:TermGenie, PMID:16756958] |
| regulation of clathrin-dependent endocytosis | biological process | Any process that modulates the frequency, rate or extent of clathrin-mediated endocytosis. [GOC:mah] |
| 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] |
| 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] |