Proteins > Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
A phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform that is encoded in the genome of human. [PRO:DNx, UniProtKB:P42336]
Synonyms
PI3-kinase subunit alpha;
PI3K-alpha;
PI3Kalpha;
PtdIns-3-kinase subunit alpha;
EC 2.7.1.137;
EC 2.7.1.153;
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha;
PtdIns-3-kinase subunit p110-alpha;
Research
Bioassay Publications (234)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 25 (10.68) | 29.6817 |
| 2010's | 162 (69.23) | 24.3611 |
| 2020's | 47 (20.09) | 2.80 |
Compounds (150)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| catechol | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| cgs 15943 | Homo sapiens (human) | IC50 | 1.2800 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 3.2119 | 26 | 35 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | Ki | 6.0000 | 1 | 1 |
| vorinostat | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| benzoin | Homo sapiens (human) | IC50 | 2,120.0000 | 2 | 2 |
| 2,6-diaminotoluene | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| anisoin | Homo sapiens (human) | IC50 | 1,170.0000 | 2 | 2 |
| gefitinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| demethoxyviridin | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| wortmannin | Homo sapiens (human) | IC50 | 8,647.2331 | 14 | 17 |
| wortmannin | Homo sapiens (human) | Ki | 0.1200 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 38.0000 | 1 | 1 |
| ku 55933 | Homo sapiens (human) | IC50 | 0.4580 | 1 | 1 |
| butein | Homo sapiens (human) | IC50 | 6.4000 | 1 | 1 |
| as 605240 | Homo sapiens (human) | IC50 | 0.1396 | 2 | 5 |
| su 11248 | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| px-866 | Homo sapiens (human) | IC50 | 0.0880 | 1 | 1 |
| nu 7026 | Homo sapiens (human) | IC50 | 13.0000 | 3 | 3 |
| 17-hydroxywortmannin | Homo sapiens (human) | IC50 | 0.0027 | 1 | 1 |
| pi103 | Homo sapiens (human) | IC50 | 0.2038 | 36 | 39 |
| PI3-Kinase alpha Inhibitor 2 | Homo sapiens (human) | IC50 | 0.1197 | 5 | 8 |
| tgx 221 | Homo sapiens (human) | IC50 | 5.2625 | 8 | 8 |
| ic 87114 | Homo sapiens (human) | IC50 | 218.3333 | 3 | 3 |
| tofacitinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pik 75 | Homo sapiens (human) | IC50 | 0.1256 | 5 | 8 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | IC50 | 0.8236 | 4 | 10 |
| nu 7441 | Homo sapiens (human) | IC50 | 1.7533 | 3 | 3 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 9.0500 | 2 | 2 |
| 5-(2,2-difluorobenzo(1,3)dioxol-5-ylmethylene)thiazolidine-2,4-dione | Homo sapiens (human) | IC50 | 4.5000 | 1 | 1 |
| quisinostat | Homo sapiens (human) | IC50 | 0.0190 | 1 | 1 |
| idelalisib | Homo sapiens (human) | IC50 | 2.4481 | 25 | 25 |
| as 252424 | Homo sapiens (human) | IC50 | 0.9400 | 1 | 1 |
| liphagal | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| zstk474 | Homo sapiens (human) | GI50 | 0.0280 | 1 | 0 |
| zstk474 | Homo sapiens (human) | IC50 | 0.0218 | 17 | 15 |
| ku-0060648 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| dactolisib | Homo sapiens (human) | IC50 | 0.0267 | 21 | 21 |
| bgt226 | Homo sapiens (human) | IC50 | 0.0040 | 2 | 2 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | IC50 | 0.0390 | 3 | 3 |
| buparlisib | Homo sapiens (human) | IC50 | 0.0550 | 19 | 19 |
| buparlisib | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| ku 0063794 | Homo sapiens (human) | IC50 | 8.9000 | 2 | 2 |
| gdc 0941 | Homo sapiens (human) | IC50 | 0.3036 | 31 | 34 |
| gdc 0941 | Homo sapiens (human) | Ki | 0.0064 | 2 | 2 |
| PP121 | Homo sapiens (human) | IC50 | 0.0520 | 2 | 2 |
| pf-04691502 | Homo sapiens (human) | IC50 | 0.0067 | 3 | 3 |
| pf-04691502 | Homo sapiens (human) | Ki | 0.0012 | 2 | 2 |
| gsk 2126458 | Homo sapiens (human) | IC50 | 0.0006 | 9 | 8 |
| gsk 2126458 | Homo sapiens (human) | Ki | 0.0000 | 2 | 1 |
| gne 477 | Homo sapiens (human) | IC50 | 0.0040 | 2 | 2 |
| gdc 0980 | Homo sapiens (human) | IC50 | 0.0049 | 2 | 2 |
| gdc 0980 | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| wye 125132 | Homo sapiens (human) | IC50 | 1.1800 | 1 | 1 |
| azd2014 | Homo sapiens (human) | IC50 | 3.8000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | IC50 | 4.5885 | 2 | 2 |
| kin-193 | Homo sapiens (human) | IC50 | 0.6067 | 3 | 3 |
| pki 402 | Homo sapiens (human) | IC50 | 0.0015 | 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 | 0.7706 | 3 | 4 |
| pki 587 | Homo sapiens (human) | IC50 | 0.0019 | 8 | 8 |
| cp 466722 | Homo sapiens (human) | IC50 | 1.4900 | 1 | 1 |
| CAY10626 | Homo sapiens (human) | IC50 | 0.0009 | 1 | 1 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | IC50 | 0.6000 | 2 | 1 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | Ki | 0.0280 | 1 | 1 |
| (3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine | Homo sapiens (human) | IC50 | 24.3333 | 3 | 3 |
| vs-5584 | Homo sapiens (human) | IC50 | 0.0119 | 2 | 2 |
| etp-46321 | Homo sapiens (human) | IC50 | 0.0043 | 3 | 3 |
| etp-46321 | Homo sapiens (human) | Ki | 0.0022 | 6 | 6 |
| gsk2292767 | Homo sapiens (human) | IC50 | 0.4664 | 3 | 3 |
| gsk2292767 | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
| gsk2269557 | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| ch 5132799 | Homo sapiens (human) | IC50 | 0.0140 | 2 | 1 |
| torin 1 | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
| ipi-145 | Homo sapiens (human) | IC50 | 4.0007 | 3 | 2 |
| gdc-0032 | Homo sapiens (human) | IC50 | 0.0099 | 4 | 3 |
| gdc-0032 | Homo sapiens (human) | Ki | 0.0002 | 4 | 3 |
| pf-4989216 | Homo sapiens (human) | IC50 | 0.0422 | 2 | 2 |
| pf-4989216 | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| torin 2 | Homo sapiens (human) | IC50 | 0.0047 | 1 | 1 |
| azd8186 | Homo sapiens (human) | IC50 | 0.4123 | 3 | 3 |
| hs-173 | Homo sapiens (human) | IC50 | 0.0023 | 3 | 3 |
| cudc-907 | Homo sapiens (human) | IC50 | 0.0246 | 7 | 7 |
| sar245408 | Homo sapiens (human) | IC50 | 0.0390 | 2 | 1 |
| byl719 | Homo sapiens (human) | IC50 | 0.0348 | 14 | 12 |
| amg 511 | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
| cc214-2 | Homo sapiens (human) | IC50 | 30.0000 | 3 | 3 |
| cc-223 | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| cc-115 | Homo sapiens (human) | IC50 | 0.8500 | 1 | 1 |
| vx-970 | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
| amg319 | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| gne-317 | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
| gne-317 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| sar405 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| bay 80-6946 | Homo sapiens (human) | IC50 | 0.0005 | 5 | 5 |
| pp242 | Homo sapiens (human) | IC50 | 1.9352 | 3 | 15 |
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
Synthesis, anticancer and antimicrobial evaluation of new benzofuran based derivatives: PI3K inhibition, quorum sensing and molecular modeling study.Bioorganic & medicinal chemistry, , 02-01, Volume: 31, 2021
Synthetic Lethality through the Lens of Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 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
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
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
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
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 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
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
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinase α (PI3Kα) inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 20, Issue:9, 2012
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
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 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
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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
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
Iodine catalyzed three component synthesis of 1-((2-hydroxy naphthalen-1-yl)(phenyl)(methyl))pyrrolidin-2-one derivatives: Rationale as potent PI3K inhibitors and anticancer agents.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.European journal of medicinal chemistry, , Volume: 60, 2013
Viridin analogs derived from steroidal building blocks.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
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
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
A stabilized demethoxyviridin derivative inhibits PI3 kinase.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Slow self-activation enhances the potency of viridin prodrugs.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Covalent reactions of wortmannin under physiological conditions.Chemistry & biology, , Volume: 14, 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
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
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
Ring closure strategy leads to potent RIPK3 inhibitors.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
[no title available]ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
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
Phthalimide conjugations for the degradation of oncogenic PI3K.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.Bioorganic & medicinal chemistry, , 02-01, Volume: 26, Issue:3, 2018
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
Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.European journal of medicinal chemistry, , Mar-31, Volume: 129, 2017
[no title available]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 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
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 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
Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
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
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.Bioorganic & medicinal chemistry, , Dec-15, Volume: 22, Issue:24, 2014
Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design.ACS medicinal chemistry letters, , Feb-13, Volume: 5, Issue:2, 2014
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
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
Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors.European journal of medicinal chemistry, , Volume: 57, 2012
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 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
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 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 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
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
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 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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.Science (New York, N.Y.), , Oct-31, Volume: 302, Issue:5646, 2003
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
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
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
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
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
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
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
[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
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
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
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
[no title available]Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 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
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
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
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
[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
Identification of highly potent and selective PI3Kδ inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 27, Issue:13, 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
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
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
Phthalimide conjugations for the degradation of oncogenic PI3K.European journal of medicinal chemistry, , May-10, Volume: 151, 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
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
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
Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
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],
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, , 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
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, 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
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
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, 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
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 and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.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
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
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 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
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.ACS medicinal chemistry letters, , Apr-09, Volume: 6, Issue:4, 2015
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
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]ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 74, 2022
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
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
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
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
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 antiproliferative activity evaluation of m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
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
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
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
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 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
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, 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
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
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
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
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
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
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
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
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
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 and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
[no title available]ACS medicinal chemistry letters, , Nov-11, Volume: 12, Issue:11, 2021
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
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 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
[no title available],
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
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
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 Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
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 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]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.European journal of medicinal chemistry, , Mar-31, Volume: 129, 2017
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
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
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
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
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
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 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.Bioorganic & medicinal chemistry, , 02-15, Volume: 32, 2021
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
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.ACS medicinal chemistry letters, , Nov-14, Volume: 10, Issue:11, 2019
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],
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
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
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
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 of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.Journal of medicinal chemistry, , 12-22, Volume: 65, Issue:24, 2022
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
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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],
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
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
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
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3Kα inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
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
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
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 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
[no title available]ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.Bioorganic & medicinal chemistry, , 05-01, Volume: 25, Issue:9, 2017
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],
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.Journal of medicinal chemistry, , Jul-09, Volume: 58, Issue:13, 2015
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
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
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.Journal of medicinal chemistry, , Jul-09, Volume: 58, Issue:13, 2015
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
[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
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
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 10 target(s):
| Target | Category | Definition |
|---|
| 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] |
| protein kinase activator activity | molecular function | Binds to and increases the activity of a protein kinase, an enzyme which phosphorylates a protein. [GOC:ai] |
| 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 4 target(s):
| Target | Category | Definition |
|---|
| 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] |
| intercalated disc | cellular component | A complex cell-cell junction at which myofibrils terminate in cardiomyocytes; mediates mechanical and electrochemical integration between individual cardiomyocytes. The intercalated disc contains regions of tight mechanical attachment (fasciae adherentes and desmosomes) and electrical coupling (gap junctions) between adjacent cells. [GOC:mtg_muscle, PMID:11732910] |
| lamellipodium | cellular component | A thin sheetlike process extended by the leading edge of a migrating cell or extending cell process; contains a dense meshwork of actin filaments. [ISBN:0815316194] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
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 3 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] |
| 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 50 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] |
| liver development | biological process | The process whose specific outcome is the progression of the liver over time, from its formation to the mature structure. The liver is an exocrine gland which secretes bile and functions in metabolism of protein and carbohydrate and fat, synthesizes substances involved in the clotting of the blood, synthesizes vitamin A, detoxifies poisonous substances, stores glycogen, and breaks down worn-out erythrocytes. [GOC:add, ISBN:068340007X] |
| regulation of protein phosphorylation | biological process | Any process that modulates the frequency, rate or extent of addition of phosphate groups into an amino acid in a protein. [GOC:hjd] |
| vasculature development | biological process | The process whose specific outcome is the progression of the vasculature over time, from its formation to the mature structure. The vasculature is an interconnected tubular multi-tissue structure that contains fluid that is actively transported around the organism. [GOC:dph, UBERON:0002409] |
| glucose metabolic process | biological process | The chemical reactions and pathways involving glucose, the aldohexose gluco-hexose. D-glucose is dextrorotatory and is sometimes known as dextrose; it is an important source of energy for living organisms and is found free as well as combined in homo- and hetero-oligosaccharides and polysaccharides. [ISBN:0198506732] |
| phagocytosis | biological process | A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732] |
| epidermal growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to the tyrosine kinase receptor EGFR (ERBB1) on the surface of a cell. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| insulin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of the insulin receptor binding to insulin. [GOC:ceb] |
| positive regulation of lamellipodium assembly | biological process | Any process that increases the rate, frequency or extent of the formation of a lamellipodium, a thin sheetlike extension of the surface of a migrating cell. [GOC:dph, GOC:tb] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| response to activity | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an activity stimulus. [GOC:mtg_muscle] |
| response to muscle inactivity | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a muscle inactivity stimulus. [GOC:mtg_muscle] |
| negative regulation of macroautophagy | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of macroautophagy. [GOC:go_curators] |
| actin cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:dph, GOC:jl, GOC:mah] |
| 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/] |
| negative regulation of actin filament depolymerization | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of actin depolymerization. [GOC:mah] |
| T cell costimulation | biological process | The process of providing, via surface-bound receptor-ligand pairs, a second, antigen-independent, signal in addition to that provided by the T cell receptor to augment T cell activation. [ISBN:0781735149] |
| positive regulation of TOR signaling | biological process | Any process that activates or increases the frequency, rate or extent of TOR signaling. [GOC:mah] |
| cellular response to insulin stimulus | 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 an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
| response to muscle stretch | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a myofibril being extended beyond its slack length. [GOC:BHF, GOC:vk, PMID:14583192] |
| vascular endothelial growth factor signaling pathway | biological process | The series of molecular signals initiated by vascular endothelial growth factor (VEGF) binding its receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, PMID:17470632] |
| regulation of multicellular organism growth | biological process | Any process that modulates the frequency, rate or extent of growth of the body of an organism so that it reaches its usual body size. [GOC:dph, GOC:ems, GOC:tb] |
| response to L-leucine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a L-leucine stimulus. [GOC:mlg] |
| anoikis | biological process | Apoptosis triggered by inadequate or inappropriate adherence to substrate e.g. after disruption of the interactions between normal epithelial cells and the extracellular matrix. [GOC:jl, http://www.copewithcytokines.de/] |
| regulation of cellular respiration | biological process | Any process that modulates the frequency, rate or extent of cellular respiration, the enzymatic release of energy from organic compounds. [GOC:jl] |
| 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] |
| negative regulation of neuron apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
| endothelial cell migration | biological process | The orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:go_curators] |
| phosphatidylinositol phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol phosphate. [ISBN:0198506732] |
| insulin-like growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| positive regulation of smooth muscle cell proliferation | biological process | Any process that activates or increases the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| T cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add] |
| 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] |
| relaxation of cardiac muscle | biological process | The process in which the extent of cardiac muscle contraction is reduced. [GOC:ecd] |
| cardiac muscle contraction | biological process | Muscle contraction of cardiac muscle tissue. [GOC:dph] |
| adipose tissue development | biological process | The process whose specific outcome is the progression of adipose tissue over time, from its formation to the mature structure. Adipose tissue is specialized tissue that is used to store fat. [GOC:dph] |
| cellular response to glucose stimulus | 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 glucose stimulus. [GOC:mah] |
| cellular response to hydrostatic pressure | 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 hydrostatic pressure stimulus. Hydrostatic pressure is the force acting on an object in a system where the fluid is at rest (as opposed to moving). The weight of the fluid above the object creates pressure on it. [GOC:mah] |
| response to dexamethasone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a dexamethasone stimulus. [GOC:mah, GOC:yaf] |
| cardiac muscle cell contraction | biological process | The actin filament-based process in which cytoplasmic actin filaments slide past one another resulting in contraction of a cardiac muscle cell. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11] |
| energy homeostasis | biological process | Any process involved in the balance between food intake (energy input) and energy expenditure. [GOC:yaf, PMID:15919751] |
| regulation of actin filament organization | biological process | Any process that modulates the frequency, rate or extent of actin filament organization. [GOC:kmv] |
| autosome genomic imprinting | biological process | The establishment of epigenetic modifications (imprints) in autosomal (non-sexual) chromosomes during gametogenesis, and propagation of these imprints during the organism's life. Genomic imprinting leads to an asymmetry between the maternal and paternal alleles and differential expression of the corresponding alleles. This can happen through heterochromatin formation or differential chromatin loop formation. [PMID:31782494] |
| response to butyrate | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a butyrate stimulus. [GO_REF:0000071, GOC:mr, GOC:TermGenie, PMID:9734870] |
| positive regulation of protein localization to membrane | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to membrane. [GO_REF:0000058, GOC:bc, GOC:PARL, GOC:TermGenie, PMID:26911690] |
| 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] |
| negative regulation of anoikis | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of anoikis. [GOC:obol] |
| 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] |
| 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] |