Page last updated: 2024-08-07 17:31:00
ALK tyrosine kinase receptor
An ALK tyrosine kinase receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9UM73]
Synonyms
EC 2.7.10.1;
Anaplastic lymphoma kinase
Research
Bioassay Publications (121)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.83) | 18.2507 |
| 2000's | 10 (8.26) | 29.6817 |
| 2010's | 83 (68.60) | 24.3611 |
| 2020's | 27 (22.31) | 2.80 |
Compounds (139)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ceritinib | Homo sapiens (human) | CC50 | 0.0543 | 6 | 6 |
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Virtual screening and further development of novel ALK inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 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
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
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
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.Journal of natural products, , Jan-24, Volume: 77, Issue:1, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
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
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 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
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
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Virtual screening and further development of novel ALK inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Virtual screening and further development of novel ALK inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
[no title available],
Identification of non-ATP-competitive α-carboline inhibitors of the anaplastic lymphoma kinase.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.Bioorganic chemistry, , Volume: 65, 2016
Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 63, 2022
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.RSC medicinal chemistry, , Nov-16, Volume: 13, Issue:11, 2022
Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 66, 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
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 29, Issue:7, 2019
[no title available]European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib.ACS medicinal chemistry letters, , Sep-13, Volume: 9, Issue:9, 2018
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
[no title available]European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer.MedChemComm, , Oct-01, Volume: 8, Issue:10, 2017
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
First macrocyclic 3European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.Bioorganic chemistry, , Volume: 65, 2016
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oJournal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.Journal of medicinal chemistry, , Feb-27, Volume: 57, Issue:4, 2014
Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 2011
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Development and Therapeutic Potential of NUAKs Inhibitors.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
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
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
[no title available]Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 12-01, Volume: 53, 2021
Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects.Bioorganic & medicinal chemistry, , 10-01, Volume: 47, 2021
Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK).Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).Journal of medicinal chemistry, , 08-25, Volume: 59, Issue:16, 2016
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
[no title available]Bioorganic & medicinal chemistry, , 07-15, Volume: 66, 2022
Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
[no title available]European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Discovery of a PROTAC targeting ALK with in vivo activity.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.Bioorganic & medicinal chemistry, , 05-01, Volume: 37, 2021
Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects.Bioorganic & medicinal chemistry, , 10-01, Volume: 47, 2021
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Design, synthesis of orally bioavailable novel anaplastic lymphoma kinase (ALK) inhibitor diphenylaminopyrimidine analogs and efficacy study on NCI-H2228 xenografts mice model.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
[no title available]European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Discovery of a potent dual ALK and EGFR T790M inhibitor.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety for anaplastic lymphoma kinase (ALK) inhibitor.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 27, Issue:10, 2017
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 25, Issue:18, 2015
Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib.ACS medicinal chemistry letters, , Sep-13, Volume: 9, Issue:9, 2018
Lipophilic Efficiency as an Important Metric in Drug Design.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
First macrocyclic 3European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oJournal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
| 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] |
| heparin binding | molecular function | Binding to heparin, a member of a group of glycosaminoglycans found mainly as an intracellular component of mast cells and which consist predominantly of alternating alpha-(1->4)-linked D-galactose and N-acetyl-D-glucosamine-6-sulfate residues. [GOC:jl, ISBN:0198506732] |
| receptor signaling protein tyrosine kinase activator activity | molecular function | Binds to and increases the activity of a receptor signaling protein tyrosine kinase. [GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
Located In
This protein is located 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] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 1 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] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 20 target(s):
| Target | Category | Definition |
|---|
| 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] |
| phosphorylation | biological process | The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732] |
| hippocampus development | biological process | The progression of the hippocampus over time from its initial formation until its mature state. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0878937420, UBERON:0002421] |
| adult behavior | biological process | Behavior in a fully developed and mature organism. [GOC:mah, ISBN:0877797099] |
| swimming behavior | biological process | The response to external or internal stimuli that results in the locomotory process of swimming. Swimming is the self-propelled movement of an organism through the water. [GOC:cvs, PMID:16764679] |
| peptidyl-tyrosine autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own tyrosine amino acid residues, or a tyrosine residue on an identical protein. [PMID:10037737, PMID:10068444, PMID:10940390] |
| regulation of apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| neuron development | biological process | The process whose specific outcome is the progression of a neuron over time, from initial commitment of the cell to a specific fate, to the fully functional differentiated cell. [GOC:dph] |
| negative regulation of lipid catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
| positive regulation of NF-kappaB transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of the transcription factor NF-kappaB. [GOC:dph, GOC:tb, PMID:15087454, PMID:15170030] |
| regulation of dopamine receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of a dopamine receptor signaling pathway activity. A dopamine receptor signaling pathway is the series of molecular signals generated as a consequence of a dopamine receptor binding to one of its physiological ligands. [GOC:dph] |
| response to environmental enrichment | 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 the provision of a combination of complex inanimate and social stimulations in the organism's housing environment. [GOC:sl, PMID:23644055, PMID:25934034] |
| energy homeostasis | biological process | Any process involved in the balance between food intake (energy input) and energy expenditure. [GOC:yaf, PMID:15919751] |
| positive regulation of dendrite development | biological process | Any process that activates or increases the frequency, rate or extent of dendrite development. [GOC:TermGenie] |
| regulation of neuron differentiation | biological process | Any process that modulates the frequency, rate or extent of neuron differentiation. [GOC:go_curators] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |