321 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28249207	78	Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.	East China Normal University
28140585	52	Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.	High Magnetic Field Laboratory
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	AbbVie Bioresearch Center
26169764	48	Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
28254166	81	Discovery of novel BTK inhibitors with carboxylic acids.	Merck & Co. Inc
27912175	14	Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.	Dalian Medical University
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University of Sydney
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck & Co.
27956037	8	Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.	Dalian Medical University
27994757	41	Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.	Pvt. Ltd.
27994736	28	Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a	Dalian Medical University
27583770	82	Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke	Bristol-Myers Squibb Research and Development
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27210433	10	Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
26976214	15	Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.	KBP Biosciences
26951753	336	Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.	Novartis Institutes for BioMedical Research
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
26630553	9	Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.	Chinese Academy of Sciences
26675441	46	Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.	Genentech
26396685	19	Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.	Amgen Inc
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26320619	88	Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).	Bristol-Myers Squibb Pharmaceutical Research Institute
26344595	26	Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.	Xi'an Jiaotong University
26277759	31	Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.	China Pharmaceutical University
26258521	104	Development of Selective Covalent Janus Kinase 3 Inhibitors.	Harvard Medical School
26087137	30	Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.	Takeda California Inc
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 Inc
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
25872980	21	TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.	Carna Biosciences, Inc
25701252	54	Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.	Genentech
25596757	64	Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.	China Pharmaceutical University
25630223	5	Target engagement in lead generation.	Eli Lilly and Company
25589924	6	Novel Disubstituted Pyrimidines as Inhibitors of Bruton's Tyrosine Kinase.	Dart Neuroscience LLC
25515957	33	Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
25466710	14	Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.	Hoffmann-La Roche Inc
24915291	73	Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.	Peking University
24731277	2	Small chemicals with inhibitory effects on PtdIns(3,4,5)P3 binding of Btk PH domain.	Konkuk University
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research and Development
24900590	55	Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.	GlaxoSmithKline
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
23442188	4	A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.	Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences
23312943	166	Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer Inc
23312472	129	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer Inc
21429745	49	3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.	GlaxoSmithKline
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma BV
22726925	216	Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.	Cellzome Ltd
23098091	91	Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.	Pfizer Inc
24900538	27	Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.	TBA
22394077	19	Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.	Hoffmann-La Roche Inc
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen Inc
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 Inc
19716697	110	The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.	Boehringer Ingelheim Pharmaceuticals Inc
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
18321716	7	ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.	Institute of Molecular Physiology
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
17684099	4	The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.	Center for Molecular Medicine of the Austrian Academy of Sciences
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
18278858	93	Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen Inc
22119469	107	Novel and selective spiroindoline-based inhibitors of Sky kinase.	Pfizer Inc
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
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	Rhône-Poulenc Rorer
21958547	108	Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.	Pfizer Inc
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21936542	143	Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.	Novartis Institute for BioMedical Research
21733693	7	Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.	GlaxoSmithKline
21620699	51	Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.	Pfizer Inc
21391610	139	Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.	Vertex Pharmaceuticals Inc
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research and Development
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen Inc
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
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	Wyeth Research
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	CGI Pharmaceuticals, Inc.
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
19019675	52	Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?	Pfizer Inc
18993068	75	Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.	Amgen Inc
18667312	24	Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.	The Scripps Research Institute
17499505	78	Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.	Boehringer Ingelheim Pharmaceuticals Inc
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen Inc
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen Inc
16686533	89	Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.	Boehringer Ingelheim Pharmaceuticals Inc
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals Inc
32832028	47	Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.	Genentech
30893553	62	Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).	Bristol-Myers Squibb Research and Development
31866272	17	Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.	Dalian Medical University
31879210	2	Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.	Yale University
31843459	57	Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.	Chia Tai Tianqing Pharmaceutical Group Co., Ltd
31830635	74	Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).	Peking University
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck & Co.
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck and Co.
27429068	54	Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.	GlaxoSmithKline R&D
27578246	158	Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.	GlaxoSmithKline R&D
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
30605829	24	Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3K?.	China Pharmaceutical University
31381333	302	Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.	TBA
30562697	84	The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.	University of Silesia in Katowice
31221612	20	Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.	East China University of Science & Technology
31138459	50	Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.	Biogen Inc.
30655951	83	Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.	Pfizer Inc.
30532965	81	Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.	GlaxoSmithKline R&D
29522671	80	Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.	Chinese Academy of Sciences
28528303	171	Discovery of a potent dual ALK and EGFR T790M inhibitor.	Harvard Medical School
31693351	473	Discovery of 4	TBA
31368705	57	Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.	Merck KGaA
30522954	11	Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.	Shanghai Institute of Pharmaceutical Industry
31234030	38	Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.	Nankai University
32083858	145	Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.	TBA
31550151	17	The Exploration of Chirality for Improved Druggability within the Human Kinome.	University of Arkansas for Medical Sciences
30939001	1	Synthetic Approaches to the New Drugs Approved During 2017.	Seattle Genetics, Inc.
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
30565923	34	Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.	Eberhard Karls University T£bingen
31395509	43	Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.	Peking University Health Science Center
31077998	81	Targeting tropomyosin receptor kinase for cancer therapy.	China Pharmaceutical University
30999237	90	Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).	Peking University
30927566	52	Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.	Shenyang Pharmaceutical University
30875504	34	Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.	Sichuan University and Collaborative Innovation Center
31260299	14	Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.	Tsinghua University
30508668	62	Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation.	China Pharmaceutical University
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
30343954	16	Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.	Eppley Institute for Research in Cancer and Allied Diseases
31526603	379	Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.	Takeda Pharmaceutical Company Limited
30857748	1	Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.	Shandong University
30857747	8	A potent seven-membered cyclic BTK (Bruton's tyrosine Kinase) chiral inhibitor conceived by structure-based drug design to lock its bioactive conformation.	Hoffmann-La Roche Ltd.
28139931	85	Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.	Pfizer Inc.
26505898	123	Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.	Novartis Institutes for Biomedical Research
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
28986130	11	Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents.	Dalian Medical University
30423248	226	Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.	Pfizer Inc.
30290988	31	Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.	EMD Serono Research & Development Institute, Inc.
30243592	23	Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.	EMD Serono Research & Development Institute, Inc.
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
29146136	32	Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.	The First Affiliated Hospital of Dalian Medical University
30139575	98	Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.	China Pharmaceutical University
30122225	25	Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.	EMD Serono Research & Development Institute, Inc.
30097367	96	Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.	Bristol-Myers Squibb Company
30082069	359	ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.	Vertex Pharmaceuticals Inc
30077608	24	Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3K?.	China Pharmaceutical University
30006143	14	Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.	Dalian Medical University
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals, Inc
29567295	19	Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors.	Shanghai Institute of Pharmaceutical Industry
30216722	77	Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.	Carna Biosciences, Inc.
30034582	72	Covalent Inhibitors of the TEC Family of Kinases and Their Methods of Use.	Temple University School of Pharmacy
28947935	5	Bruton's Tyrosine Kinase Inhibitors for the Treatment of Autoimmune Diseases and Cancers.	AMRI
28131712	30	Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).	Integral BioSciences, Pvt. Ltd.
29715023	56	Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.	China Pharmaceutical University
29198867	46	Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.	Carna Biosciences, Inc.
28279528	53	Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.	Advinus Therapeutics Ltd
29631132	33	The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.	Shaanxi University of Science & Technology
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science and Technology (KIST)
28628824	98	Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.	University of Science and Technology of China
29852068	86	Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.	Eberhard Karls University T£bingen
28734581	37	Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.	Sichuan University and Collaborative Innovation Center
28720503	146	Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.	Merck & Co.
28432946	13	Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.	Dalian Medical University
28282122	9	Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.	High Magnetic Field Laboratory
28259529	31	Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.	The Ohio State University
28927786	52	Discovery of highly potent, selective, covalent inhibitors of JAK3.	Bristol-Myers Squibb Research and Development
28337328	6	Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.	Dana-Farber Cancer Institute Inc
28626519	48	Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.	Genentech
28438385	24	Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth.	Indiana University School of Medicine
28956923	34	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 Mutants in FLT3-ITD Positive AML.	Chinese Academy of Sciences
28408223	5	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.	IntelliSyn Pharma
28315597	85	Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.	University of Science and Technology of China
29457982	80	Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.	Genentech
28945083	33	In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.	National Institute of Biological Sciences, Beijing
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34414360	60	Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.	The University of Arizona
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21612376	6	Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine.	GITAM University
21438710	18	Oxamic acid analogues as LDH-C4-specific competitive inhibitors.	Instituto Politécnico Nacional
24047900	19	Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.	Vanderbilt University
20962348	17	Probing the active site of the deoxynucleotide N-hydrolase Rcl encoded by the rat gene c6orf108.	Institut Pasteur
14564311	4	Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.	University of Maryland Hospital
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10374926	2	Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.	Hungarian Academy of Sciences
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8996185	121	Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.	Synthélabo Recherche
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15696597	18	Structure-aided optimization of kinase inhibitors derived from alsterpaullone.	Technische Universität Braunschweig
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7996470	29	The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.	University of Michigan
2968449	13	Characterization of [5,6-3H]SQ 29,548 as a high affinity radioligand, binding to thromboxane A2/prostaglandin H2-receptors in human platelets.	Squibb Institute for Medical Research
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2139469	31	Characterization of D1 dopamine receptors in the bovine pineal gland with [3H]SCH 23390.	University of Nebraska
18804036	24	Structure-guided development of efficacious antifungal agents targeting Candida glabrata dihydrofolate reductase.	University of Connecticut
15293988	1	A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.	Virginia Commonwealth University
18722768	10	Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.	Anadys Pharmaceuticals
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19477642	87	Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.	GSK
19167883	5	Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.	Gilead Sciences Inc
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15857113	12	Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.	GSK
17709247	33	Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.	Amgen Inc
15755665	7	Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.	Pfizer Inc
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15466206	10	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.	Bayer Pharmaceuticals Corporation
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15582402	9	Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).	University of Illinois at Chicago
17451235	19	Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.	Astex
14592490	80	Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.	Merck Research Laboratories
16942016	27	Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.	University of Kansas
15887974	10	Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.	Universidad Central de Venezuela
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10866371	12	Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.	GlaxoSmithKline
15743198	134	Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.	Saarland University
16392787	16	Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.	Burnham Institute
11266159	63	3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).	SmithKline Beecham Pharmaceuticals Ltd
15771433	30	Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.	Johnson & Johnson Pharmaceutical
8568816	69	Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor	Parke-Davis Pharmaceutical Research
8642565	36	Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.	Sandoz Research Institute
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