The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28359790 |
110 |
Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors. |
Takeda California |
| 28103025 |
29 |
Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277. |
Korea University |
| 26914985 |
124 |
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. |
Boehringer Ingelheim Rcv |
| 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 |
| 26483198 |
30 |
Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-ß type I receptor kinase. |
Ewha Womans University |
| 25101911 |
95 |
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
Massachusetts Institute of Technology |
| 24786585 |
200 |
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. |
Ewha Womans University |
| 24704197 |
32 |
4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-ß type I receptor kinase. |
Ewha Womans University |
| 24055046 |
11 |
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles as inhibitors of transforming growth factor-ß type I receptor (ALK5). |
Capital Normal University |
| 23639540 |
89 |
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. |
Vanderbilt University Medical Center |
| 24900673 |
1 |
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. |
Glaxosmithkline |
| 23294702 |
6 |
Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-ß type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 23117174 |
74 |
5-(1,3-Benzothiazol-6-yl)-4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazole derivatives as potent and selective transforming growth factor-ß type I receptor inhibitors. |
Taisho Pharmaceutical |
| 23130626 |
46 |
Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFß signaling. |
Human Biomolecular Research Institute |
| 22542194 |
22 |
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring. |
Pfizer |
| 21911290 |
76 |
Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-ß type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 16570917 |
32 |
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
Glaxosmithkline |
| 22325945 |
55 |
Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor-ß type I receptor kinase. |
Taisho Pharmaceutical |
| 22310227 |
89 |
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. |
Glaxosmithkline |
| 21696866 |
36 |
Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-ß type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 21733693 |
7 |
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. |
Glaxosmithkline |
| 21435890 |
38 |
Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 21341675 |
266 |
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. |
Glaxosmithkline |
| 20919678 |
109 |
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI). |
Boehringer Ingelheim Pharma |
| 20472445 |
23 |
Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 20176484 |
23 |
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists. |
Northeastern Ohio Universities Colleges of Medicine and Pharmacy |
| 19914068 |
66 |
Pyrazolone based TGFbetaR1 kinase inhibitors. |
Biogen Idec |
| 19640613 |
104 |
Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors. |
Sichuan University |
| 19616940 |
2 |
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5). |
Institute of Pharmacology and Toxicology |
| 19285388 |
41 |
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. |
Glaxosmithkline |
| 19135364 |
38 |
2-Aminoimidazoles inhibitors of TGF-beta receptor 1. |
Abbott Laboratories |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
| 18479116 |
8 |
Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase. |
Kirin Pharma |
| 17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
| 17552507 |
21 |
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
Ewha Womans University |
| 17289388 |
8 |
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors. |
Tibotec |
| 16539403 |
78 |
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. |
Eli Lilly |
| 15317461 |
53 |
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. |
Glaxosmithkline |
| 14643325 |
3 |
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI). |
Biogen |
| 12954047 |
80 |
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. |
Eli Lilly |
| 11855979 |
13 |
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). |
Glaxosmithkline |
| 32787083 |
172 |
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. |
Ontario Institute For Cancer Research |
| 32631540 |
29 |
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-? (TGF-?) type I receptor inhibitors. |
China Pharmaceutical University |
| 31810777 |
18 |
Synthesis and evaluation of the HIF-1? inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
Yanbian University |
| 31303386 |
35 |
Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
Yanbian University |
| 27460209 |
152 |
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors. |
Takeda California |
| 32369358 |
143 |
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma. |
University of Toronto |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 31408333 |
2 |
Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor ? Type I Receptor. |
Sun Yat-Sen University |
| 31299584 |
32 |
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
Yanbian University |
| 32071685 |
40 |
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent. |
Bristol-Myers Squibb Research & Development |
| 30530193 |
64 |
Targeting the immunity protein kinases for immuno-oncology. |
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 |
| 31749904 |
74 |
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors. |
Glaxosmithkline |
| 26288266 |
4 |
Medicinal Chemistry Approaches to Heart Regeneration. |
Tu Dortmund University |
| 28135685 |
91 |
ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
Palack£ |
| 30429955 |
44 |
Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents. |
Bristol-Myers Squibb Research and Development |
| 30227946 |
58 |
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors. |
National Center For Advancing Translational Sciences |
| 30085668 |
41 |
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept. |
Institute of Cancer Research |
| 29422332 |
51 |
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGF?RI). |
Bristol-Myers Squibb |
| 28162900 |
7 |
Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor. |
University of Toronto |
| 22512727 |
20 |
Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives. |
Inonu University |
| 12714592 |
8 |
Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155. |
Schering-Plough Research Institute |
| 12438526 |
1 |
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. |
Merck Research Laboratories |
| 7535424 |
29 |
Characterization of somatostatin receptor subtypes controlling rat gastric acid and pancreatic amylase release. |
Tulane University |
| 21791013 |
5 |
A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors. |
Sanford-Burnham Medical Research Institute |
| 19628388 |
35 |
Benzo[c][2,7]naphthyridines as inhibitors of PDK-1. |
Wyeth Research |
| 17993277 |
42 |
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. |
Universite Paris 7-Denis Diderot |
| 18269228 |
93 |
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. |
Wyeth Research |
| 15293984 |
11 |
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site. |
University of Michigan |
| 7932546 |
5 |
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. |
Upjohn |
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