233 articles for thisTarget

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PMID	Data	Article Title	Organization
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
28159414	15	The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity.	Osaka Prefecture University
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27856237	11	Synthesis, anticancer, and docking studies of salicyl-hydrazone analogues: A novel series of small potent tropomyosin receptor kinase A inhibitors.	Dongguk University
27779399	22	Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.	Eli Lilly
27299736	37	The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.	St. John'S University
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27003761	120	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.	Nerviano Medical Sciences
27117263	51	Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.	Takeda Pharmaceutical
26995531	32	Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.	The University of Tokyo
26771245	7	Recent developments of 2-aminothiazoles in medicinal chemistry.	Sree Chaitanya College
26762835	342	Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).	Icahn School of Medicine At Mount Sinai
26442778	15	Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.	Institute For Basic Science (Ibs)
26431428	36	Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).	Wuxi Apptec
26222319	192	Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.	Nerviano Medical Sciences
26071372	89	Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.	Astellas Pharma
26121481	37	Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.	Vertex Pharmaceuticals
26005534	158	(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.	Genomics Institute of The Novartis Research Foundation
25835317	63	Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.	Sichuan University
25791677	15	Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.	Zhengzhou University
25723005	111	The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.	TBA
25454499	6	Design and nuclear magnetic resonance (NMR) structure determination of the second extracellular immunoglobulin tyrosine kinase A (TrkAIg2) domain construct for binding site elucidation in drug discovery.	Southmead Hospital
25068800	34	UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.	University of North Carolina At Chapel Hill
25022204	78	Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.	Universit£
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24914455	38	Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.	Merck Research Laboratories
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24819116	135	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 oncogene 1 (ROS1) with preclinical brain expo	Pfizer
24432909	13	Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.	Pfizer
24359159	60	Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.	Astrazeneca
24900767	3	Inhibitors of Tropomyosin-Receptor Kinases (Trk's): Potential Pain Therapy and More.	Therachem Research Medilab (India)
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
23742252	81	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-diamine (LDK378) currently in phase 1 and phase	Genomics Institute of The Novartis Research Foundation
23570792	61	SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.	Emd-Serono Research Institute
23312472	129	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
21381769	56	Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.	Universite£
23061660	92	Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.	Genentech
22827572	67	Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).	Glaxosmithkline
22039836	188	Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).	Johnson & Johnson Pharmaceutical Research & Development
24900538	27	Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.	TBA
22575050	40	Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities.	Korea Advanced Institute of Science and Technology (Kaist)
22795331	51	Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.	Janssen Pharmaceutical Companies of Johnson & Johnson
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
24900443	158	Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.	TBA
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
22148921	48	Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c	Cephalon
21608528	166	Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.	Merck Research Laboratories
21138246	44	Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.	Astrazeneca R&D
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20153204	109	Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.	Nerviano Medical Sciences
19716697	110	The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.	Boehringer Ingelheim Pharmaceuticals
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19320489	125	Discovery and development of aurora kinase inhibitors as anticancer agents.	Vertex Pharmaceuticals
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18508265	13	TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone.	Cephalon
18342505	43	Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
11931608	17	Inhibition of protein-protein association by small molecules: approaches and progress.	Pfizer
15013000	31	Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.	Glaxosmithkline
22040023	63	Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).	Pfizer
22154349	123	5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.	Nerviano Medical Sciences
22119469	107	Novel and selective spiroindoline-based inhibitors of Sky kinase.	Pfizer
22014550	337	Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).	Ansaris
22001029	28	Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors.	Korea Research Institute of Chemical Technology
21958544	31	Indolin-2-one p38a inhibitors III: bioisosteric amide replacement.	RhôNe-Poulenc Rorer
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21812414	106	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).	Pfizer
21493067	22	In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.	Astrazeneca R&D Boston
21470862	110	NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.	Nerviano Medical Sciences
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
19039322	50	Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.	Center For Molecular Medicine of The Austrian Academy of Sciences
20655209	18	Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.	Université
20397705	208	Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.	Nerviano Medical Sciences
20382527	26	Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.	Bristol-Myers Squibb Research and Development
20361800	22	5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.	Institute of Science and Technology
20346655	117	Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.	Abbott Laboratories
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19857966	62	Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.	Astrazeneca R&D Boston
18289854	44	Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.	Bristol-Myers Squibb Research and Development
18242992	30	Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.	Johnson & Johnson Pharmaceutical Research & Development
18055203	51	Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.	Bristol-Myers Squibb Research and Development
17239587	43	1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.	Cephalon
15916429	11	Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.	Cephalon
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
14640546	46	A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin	Cephalon
12270156	8	Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.	Cephalon
11755341	50	Mixed lineage kinase activity of indolocarbazole analogues.	Kyowa Hakko Kogyo
32292564	138	Efficacy and Tolerability of Pyrazolo[1,5-	The Genomics Institute of The Novartis Research Foundation
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
27531604	55	Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).	Bristol-Myers Squibb Research and Development
27379978	140	4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.	Chinese Academy of Sciences
27219676	60	Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.	Chinese Academy of Sciences
30755337	95	Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.	Japan Tobacco
31310125	83	2-Amino-2,3-dihydro-1	Jinan University
31444087	90	Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA).	Zoetis
31009559	50	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.	Takeda Pharmaceutical
31721578	44	Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.	National Health Research Institutes
31693351	473	Discovery of 4	TBA
31677447	44	Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.	Central China Normal University
32298114	14	Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.	Universit£
31271959	76	Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.	Chinese Academy of Sciences
31103903	47	Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.	China Pharmaceutical University
31235262	37	The discovery of novel 3-aryl-indazole derivatives as peripherally restricted pan-Trk inhibitors for the treatment of pain.	Asahi Kasei Pharma
31077998	81	Targeting tropomyosin receptor kinase for cancer therapy.	China Pharmaceutical University
31699609	5	An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue.	Osaka Prefecture University
30763817	39	Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.	University of Naples Federico Ii
30987781	88	Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.	Southeast University
30600206	3	Discovery of an isocoumarin analogue that modulates neuronal functions via neurotrophin receptor TrkB.	Indian Institute of Technology Madras
30188734	41	Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.	University of Arkansas For Medical Sciences
30384048	365	ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.	University of Florida
30347329	84	Synthesis, biological evaluation, and molecular modeling of 11H-indeno[1,2-b]quinoxalin-11-one derivatives and tryptanthrin-6-oxime as c-Jun N-terminal kinase inhibitors.	Montana State University
30343954	16	Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.	Eppley Institute For Research In Cancer and Allied Diseases
9191963	12	Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.	Kyowa Hakko Kogyo
31526603	379	Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.	Takeda Pharmaceutical
31857832	51	Modulation of Tropomyosin Receptor Kinase for the Treatment of Neurotrophin Diseases: Alzheimer's, Huntington's and Parkinson's.	Usona Institute
29672039	37	Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.	Pfizer
31610943	354	Lead identification and characterization of hTrkA type 2 inhibitors.	Zoetis
26509640	234	Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.	Abbvie Bioresearch Center
26843921	39	Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies.	The University of Arizona
31200237	95	Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.	Shanghai Pharmaceuticals Holding
30978288	113	A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.	Northwestern University
30347155	155	Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.	Unc Eshelman School of Pharmacy
30480444	85	Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.	Sichuan University/Collaborative Innovation Center of Biotherapy
30460842	111	Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.	Purdue University
29944371	79	Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.	Pfizer
29746776	14	From Cancer to Pain Target by Automated Selectivity Inversion of a Clinical Candidate.	Heidelberg University
30075624	71	Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.	Jinan University
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
28929759	83	Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.	Wuxi Apptec
29518312	78	Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.	Nankai University
28465100	85	Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.	Merck
	43	Identification of inhibitors of SARS-CoV-2 3CL-Pro enzymatic activity using a small molecule in-vitro repurposing screen	Fraunhofer Institute For Translational Medicine and Pharmacology (Itmp) and Fraunhofer Cluster of Excellence For Immune Mediated Diseases (Cimd
23009660	17	Structure-activity relationships of bergenin derivatives effect on a-glucosidase inhibition.	Kinki University
22524677	6	Interaction of superoxide dismutase with the glycine zipper regions of ß-amyloid peptides: is there an implication towards Alzheimer's disease and oxidative stress?	Rhodes University
23884422	10	Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation.	Mcgill University
27496071	4	Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents.	Korea Institute of Science and Technology
15665139	3	Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.	German Cancer Research Center
17373554	5	Inhibitory effect on soybean lipoxygenase and docking studies of some secondary metabolites, isolated from Origanum vulgare L. ssp. hirtum.	University of Athens
11602678	5	OPC-28326, a selective femoral vasodilator, is an alpha2C-adrenoceptor-selective antagonist.	Otsuka Maryland Research Institute
10646498	23	Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.	Janssen Research Foundation
10051134	18	[3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum.	Monash University
9928251	27	Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor.	Albany Medical College
15515092	54	The core structures of roseophilin and the prodigiosin alkaloids define a new class of protein tyrosine phosphatase inhibitors.	Max-Planck-Institut FÜR Kohlenforschung
16611213	6	Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction.	Johnson & Johnson Pharmaceutical Research & Development
21566738	3	Virtual screening for potential inhibitors of homology modeled Leptospira interrogans MurD ligase.	Svims University
1320204	1	Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285.	Centre De Pharmacologie-Endocrinologie (Montpellier, France)
16638531	16	Stable benzotriazole esters as mechanism-based inactivators of the severe acute respiratory syndrome 3CL protease.	Academia Sinica
20426425	2	Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.	University of Sheffield
18851976	4	Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.	University of Milano
18440229	175	2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.	Irbm/Merck Research Laboratories
15482949	17	Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.	Glaxosmithkline
9876115	183	Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.	University of Auckland
9622549	23	New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.	Purdue University