Proteins > Mast/stem cell growth factor receptor Kit
Page last updated: 2024-08-07 18:30:26
Mast/stem cell growth factor receptor Kit
A mast/stem cell growth factor receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P10721]
Synonyms
SCFR;
EC 2.7.10.1;
Piebald trait protein;
PBT;
Proto-oncogene c-Kit;
Tyrosine-protein kinase Kit;
p145 c-kit;
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Research
Bioassay Publications (154)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 51 (33.12) | 29.6817 |
| 2010's | 87 (56.49) | 24.3611 |
| 2020's | 16 (10.39) | 2.80 |
Compounds (142)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.Journal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Discovery of ( E)- NJournal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
[no title available]Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT KinaJournal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
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 potent and selective inhibitors of PDGF receptor autophosphorylation.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.Journal of medicinal chemistry, , Oct-06, Volume: 48, Issue:20, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
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
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
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
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
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
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
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
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
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, 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
Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.Cancer research, , Oct-01, Volume: 64, Issue:19, 2004
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & medicinal chemistry, , 03-15, Volume: 28, Issue:6, 2020
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.Leukemia, , Volume: 23, Issue:3, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.Proceedings of the National Academy of Sciences of the United States of America, , Feb-27, Volume: 104, Issue:9, 2007
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
[no title available],
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, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.Journal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
[no title available]Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT KinaJournal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.European journal of medicinal chemistry, , Jul-23, Volume: 82, 2014
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 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
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of ( E)- NJournal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Three dimensional pharmacophore modelling for c-Kit receptor tyrosine kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.Journal of molecular graphics & modelling, , Volume: 26, Issue:1, 2007
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline deriJournal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
[no title available],
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 24, Issue:4, 2014
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
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
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
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
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Three dimensional pharmacophore modelling for c-Kit receptor tyrosine kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
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
Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.Cancer research, , Sep-01, Volume: 66, Issue:17, 2006
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 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
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 N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
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
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.ACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase MutanJournal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
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
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
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
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
Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions.European journal of medicinal chemistry, , May-01, Volume: 193, 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
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.Bioorganic chemistry, , Volume: 57, 2014
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BJournal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| protease binding | molecular function | Binding to a protease or a peptidase. [GOC:hjd] |
| 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] |
| stem cell factor receptor activity | molecular function | Combining with stem cell factor (SCF) receptor ligand 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. Stem cell factor is a cytokine that stimulates mast cell growth and differentiation. [GOC:jl, GOC:signaling, PMID:10698217] |
| 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] |
| cytokine binding | molecular function | Binding to a cytokine, any of a group of proteins that function to control the survival, growth and differentiation of tissues and cells, and which have autocrine and paracrine activity. [GOC:ai, GOC:bf, ISBN:0198599471] |
| SH2 domain binding | molecular function | Binding to a SH2 domain (Src homology 2) of a protein, a protein domain of about 100 amino-acid residues and belonging to the alpha + beta domain class. [GOC:go_curators, Pfam:PF00017] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| growth factor binding | molecular function | Binding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| fibrillar center | cellular component | A structure found most metazoan nucleoli, but not usually found in lower eukaryotes; surrounded by the dense fibrillar component; the zone of transcription from multiple copies of the pre-rRNA genes is in the border region between these two structures. [PMID:10754561] |
| acrosomal vesicle | cellular component | A structure in the head of a spermatozoon that contains acid hydrolases, and is concerned with the breakdown of the outer membrane of the ovum during fertilization. It lies just beneath the plasma membrane and is derived from the lysosome. [ISBN:0124325653, ISBN:0198506732] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| 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] |
| cell-cell junction | cellular component | A cell junction that forms a connection between two or more cells of an organism; excludes direct cytoplasmic intercellular bridges, such as ring canals in insects. [GOC:aruk, GOC:bc, GOC:dgh, GOC:hb, GOC:mah, PMID:21422226, PMID:28096264] |
| external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
| cytoplasmic side of plasma membrane | cellular component | The leaflet the plasma membrane that faces the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
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 1 target(s):
| Target | Category | Definition |
|---|
| 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 71 target(s):
| Target | Category | Definition |
|---|
| ovarian follicle development | biological process | The process whose specific outcome is the progression of the ovarian follicle over time, from its formation to the mature structure. [https://www.ncbi.nlm.nih.gov/books/NBK279054/] |
| myeloid progenitor cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a myeloid progenitor cell. Myeloid progenitor cells include progenitor cells for any of the myeloid lineages. [GOC:add, PMID:16551264] |
| lymphoid progenitor cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a lymphoid progenitor cell. Lymphoid progenitor cells include progenitor cells for any of the lymphoid lineages. [GOC:add, PMID:16551251, PMID:16551264] |
| immature B cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of an immature B cell. [GOC:jal, ISBN:0781735149, PMID:16551251] |
| mast cell chemotaxis | biological process | The movement of a mast cell in response to an external stimulus. [GOC:add, PMID:11292027, PMID:12789214, PMID:16448392] |
| positive regulation of dendritic cell cytokine production | biological process | Any process that activates or increases the frequency, rate, or extent of dendritic cell cytokine production. [GOC:add] |
| glycosphingolipid metabolic process | biological process | The chemical reactions and pathways involving glycosphingolipids, any compound with residues of sphingoid and at least one monosaccharide. [ISBN:0198547684] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| 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] |
| spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
| spermatid development | biological process | The process whose specific outcome is the progression of a spermatid over time, from its formation to the mature structure. [GOC:dph, GOC:go_curators] |
| germ cell migration | biological process | The orderly movement of a cell specialized to produce haploid gametes through the embryo from its site of production to the place where the gonads will form. [GOC:bf, GOC:jl] |
| regulation of cell shape | biological process | Any process that modulates the surface configuration of a cell. [GOC:dph, GOC:go_curators, GOC:tb] |
| visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
| male gonad development | biological process | The process whose specific outcome is the progression of the male gonad over time, from its formation to the mature structure. [GOC:jid] |
| positive regulation of phospholipase C activity | biological process | Any process that increases the rate of phospholipase C activity. [GOC:dph, GOC:tb] |
| cytokine-mediated signaling pathway | biological process | The series of molecular signals initiated by the binding of a cytokine to a receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:19295629] |
| stem cell population maintenance | biological process | The process by which an organism or tissue maintains a population of stem cells of a single type. This can be achieved by a number of mechanisms: stem cell asymmetric division maintains stem cell numbers; stem cell symmetric division increases them; maintenance of a stem cell niche maintains the conditions for commitment to the stem cell fate for some types of stem cell; stem cells may arise de novo from other cell types. [GOC:mah, ISBN:0878932437] |
| lamellipodium assembly | biological process | Formation of a lamellipodium, a thin sheetlike extension of the surface of a migrating cell. [GOC:mah, ISBN:0815316194] |
| 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] |
| hemopoiesis | biological process | The process whose specific outcome is the progression of the myeloid and lymphoid derived organ/tissue systems of the blood and other parts of the body over time, from formation to the mature structure. The site of hemopoiesis is variable during development, but occurs primarily in bone marrow or kidney in many adult vertebrates. [GOC:dgh, ISBN:0198506732] |
| T cell differentiation | biological process | The process in which a precursor cell type acquires characteristics of a more mature T-cell. A T cell is a type of lymphocyte whose definin characteristic is the expression of a T cell receptor complex. [GO_REF:0000022, GOC:jid, GOC:mah] |
| erythrocyte differentiation | biological process | The process in which a myeloid precursor cell acquires specializes features of an erythrocyte. [GOC:mah] |
| melanocyte differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a melanocyte. [GOC:mah] |
| positive regulation of pseudopodium assembly | biological process | Any process that activates or increases the frequency, rate or extent of the assembly of pseudopodia. [GOC:pg] |
| positive regulation of mast cell cytokine production | biological process | Any process that activates or increases the frequency, rate, or extent of mast cell cytokine production. [GOC:mah] |
| somatic stem cell population maintenance | biological process | Any process by which an organism retains a population of somatic stem cells, undifferentiated cells in the embryo or adult which can undergo unlimited division and give rise to cell types of the body other than those of the germ-line. [GOC:bf, ISBN:0582227089] |
| embryonic hemopoiesis | biological process | The stages of blood cell formation that take place within the embryo. [GOC:bf] |
| ectopic germ cell programmed cell death | biological process | Programmed cell death of an errant germ line cell that is outside the normal migratory path or ectopic to the gonad. This is an important mechanism of regulating germ cell survival within the embryo. [PMID:12814944] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| hematopoietic stem cell migration | biological process | The orderly movement of a hematopoietic stem cell from one site to another. A hematopoietic stem cell is a cell from which all cells of the lymphoid and myeloid lineages develop, including blood cells and cells of the immune system. [CL:0000037, GOC:BHF, PMID:20234092] |
| megakaryocyte development | biological process | The process whose specific outcome is the progression of a megakaryocyte cell over time, from its formation to the mature structure. Megakaryocyte development does not include the steps involved in committing a cell to a megakaryocyte fate. A megakaryocyte is a giant cell 50 to 100 micron in diameter, with a greatly lobulated nucleus, found in the bone marrow. [CL:0000556, GOC:BHF, GOC:vk] |
| Fc receptor signaling pathway | biological process | The series of molecular signals initiated by the binding of the Fc portion of an immunoglobulin to an Fc receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. The Fc portion of an immunoglobulin is its C-terminal constant region. [GOC:phg, Wikipedia:Fc_receptor] |
| Kit signaling pathway | biological process | The series of molecular signals initiated by the binding of stem cell factor to the tyrosine kinase receptor KIT on the surface of a target cell, and ending with regulation of a downstream cellular process, e.g. transcription. Stem cell factor (KIT ligand) binding to the receptor Kit mediates receptor dimerization, activation of its intrinsic tyrosine kinase activity and autophosphorylation. The activated receptor then phosphorylates various substrates, thereby activating distinct signaling cascades within the cell that trigger a change in state or activity of the cell. [GOC:nhn, GOC:signaling, PMID:16129412] |
| erythropoietin-mediated signaling pathway | biological process | The series of molecular signals initiated by erythropoietin (EPO) binding to the erythropoietin receptor (EPO-R) on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn, PMID:12489509] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| positive regulation of tyrosine phosphorylation of STAT protein | biological process | Any process that activates or increases the frequency, rate or extent of the introduction of a phosphate group to a tyrosine residue of a STAT (Signal Transducer and Activator of Transcription) protein. [GOC:jl, PMID:11426647] |
| negative regulation of programmed cell death | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of programmed cell death, cell death resulting from activation of endogenous cellular processes. [GOC:jl] |
| mast cell degranulation | biological process | The regulated exocytosis of secretory granules containing preformed mediators such as histamine, serotonin, and neutral proteases by a mast cell. [ISBN:0781735149] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| pigmentation | biological process | The accumulation of pigment in an organism, tissue or cell, either by increased deposition or by increased number of cells. [GOC:jl] |
| tongue development | biological process | The process whose specific outcome is the progression of the tongue over time, from its formation to the mature structure. The tongue is the movable, muscular organ on the floor of the mouth of most vertebrates, in many other mammals is the principal organ of taste, aids in the prehension of food, in swallowing, and in modifying the voice as in speech. [GOC:jl, UBERON:0001723] |
| positive regulation of Notch signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the Notch signaling pathway. [GOC:go_curators] |
| positive regulation of receptor signaling pathway via JAK-STAT | biological process | Any process that activates or increases the frequency, rate or extent of the JAK-STAT signaling pathway activity. [GOC:bf] |
| response to cadmium ion | 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 cadmium (Cd) ion stimulus. [GOC:ai] |
| 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] |
| positive regulation of long-term neuronal synaptic plasticity | biological process | A process that increases long-term neuronal synaptic plasticity, the ability of neuronal synapses to change long-term as circumstances require. Long-term neuronal synaptic plasticity generally involves increase or decrease in actual synapse numbers. [GOC:jid, PMID:11891290] |
| digestive tract development | biological process | The process whose specific outcome is the progression of the digestive tract over time, from its formation to the mature structure. The digestive tract is the anatomical structure through which food passes and is processed. [GOC:go_curators] |
| stem cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a stem cell. A stem cell is a cell that retains the ability to divide and proliferate throughout life to provide progenitor cells that can differentiate into specialized cells. [CL:0000034, GOC:isa_complete] |
| epithelial cell proliferation | biological process | The multiplication or reproduction of epithelial cells, resulting in the expansion of a cell population. Epithelial cells make up the epithelium, the covering of internal and external surfaces of the body, including the lining of vessels and other small cavities. It consists of cells joined by small amounts of cementing substances. [ISBN:0721662544] |
| detection of mechanical stimulus involved in sensory perception of sound | biological process | The series of events involved in the perception of sound vibration in which the vibration is received and converted into a molecular signal. [GOC:ai] |
| positive regulation of DNA-binding transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:ai] |
| negative regulation of developmental process | biological process | Any process that stops, prevents or reduces the rate or extent of development, the biological process whose specific outcome is the progression of an 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:ai] |
| 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] |
| cell chemotaxis | biological process | The directed movement of a motile cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [GOC:dph] |
| mast cell differentiation | biological process | The process in which a relatively unspecialized myeloid precursor cell acquires the specialized features of a mast cell. A mast cell is a cell that is found in almost all tissues containing numerous basophilic granules and capable of releasing large amounts of histamine and heparin upon activation. [GOC:dph, GOC:tb] |
| mast cell proliferation | biological process | The expansion of a mast cell population by cell division. [GOC:add] |
| positive regulation of mast cell proliferation | biological process | Any process that activates or increases the rate or extent of mast cell proliferation. [GOC:add, GOC:mah] |
| melanocyte migration | biological process | The orderly movement of melanocytes from one site to another, often during the development of a multicellular organism. A melanocyte is a pigment cell derived from the neural crest. It contains melanin-filled pigment granules, which give a brown to black appearance. [CL:0000148, GOC:uh, PMID:22637532] |
| melanocyte adhesion | biological process | The attachment of a melanocyte to another cell via adhesion molecules. [CL:0000148, GOC:uh, PMID:22637532] |
| positive regulation of pyloric antrum smooth muscle contraction | biological process | Any process that increases the frequency, rate or extent of any pyloric antrum smooth muscle contraction. [GOC:sl, PMID:15890336] |
| regulation of bile acid metabolic process | biological process | Any process that modulates the frequency, rate or extent of bile acid metabolic process. [GO_REF:0000058, GOC:bf, GOC:TermGenie] |
| positive regulation of colon smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of colon smooth muscle contraction. [GO_REF:0000058, GOC:TermGenie, PMID:24170253] |
| positive regulation of small intestine smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of small intestine smooth muscle contraction. [GO_REF:0000058, GOC:TermGenie, PMID:11991626] |
| positive regulation of vascular associated smooth muscle cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of vascular smooth muscle cell differentiation. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:19088079] |
| negative regulation of reproductive process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of reproductive process. [GOC:mah] |
| positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| 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] |
| B cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a B cell. A B cell is a lymphocyte of B lineage with the phenotype CD19-positive and capable of B cell mediated immunity. [GO_REF:0000022, GOC:mah] |
| hematopoietic progenitor cell differentiation | biological process | The process in which precursor cell type acquires the specialized features of a hematopoietic progenitor cell, a class of cell types including myeloid progenitor cells and lymphoid progenitor cells. [GOC:add, GOC:rl, ISBN:0781735149, PMID:16551251] |