The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28274629 |
76 |
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism. |
Hanyang University |
28212021 |
111 |
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT |
Suven Life Sciences |
26819660 |
82 |
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor. |
Central Pharmaceutical Research Institute |
22696418 |
36 |
Evaluation of inhibition selectivity for human cytochrome P450 2A enzymes. |
University of Kansas |
22496391 |
40 |
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human. |
Bristol-Myers Squibb Research |
23132334 |
28 |
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. |
Glaxosmithkline |
25751283 |
79 |
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities. |
Purdue University |
25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£T T£Bingen |
25458499 |
78 |
Rational design of novel CYP2A6 inhibitors. |
University of Eastern Finland |
24512187 |
69 |
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
Pfizer |
24900630 |
16 |
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
University of Cape Town |
23869452 |
67 |
Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type. |
Saarland University |
23896611 |
16 |
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
University of Cape Town |
23806553 |
7 |
Discovery of triazines as potent, selective and orally active PDE4 inhibitors. |
Biocrea |
23600958 |
57 |
Pyranoflavones: a group of small-molecule probes for exploring the active site cavities of cytochrome P450 enzymes 1A1, 1A2, and 1B1. |
Xavier University of Louisiana |
16248836 |
154 |
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
F. Hoffmann-La Roche |
19110342 |
81 |
Exploring QSAR and QAAR for inhibitors of cytochrome P450 2A6 and 2A5 enzymes using GFA and G/PLS techniques. |
Jadavpur University |
23043539 |
60 |
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. |
The Institute of Cancer Research |
22651823 |
57 |
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
Pfizer |
22938786 |
86 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
Dainippon Sumitomo Pharma |
20565112 |
55 |
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. |
The Institute of Cancer Research |
18345609 |
57 |
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration. |
The Institute of Cancer Research |
17201408 |
91 |
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
Wyeth Research |
15658857 |
96 |
Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme. |
University of Kuopio |
15634016 |
232 |
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6. |
Human Biomolecular Research Institute |
22019468 |
15 |
Identification of novel CYP2A6 inhibitors by virtual screening. |
University of Eastern Finland |
21978946 |
45 |
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. |
Takeda Pharmaceutical |
21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
18598020 |
75 |
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
17933533 |
36 |
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases. |
The Institute of Cancer Research |
17705360 |
76 |
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site. |
Wyeth Research |
17399990 |
45 |
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2). |
Université |
32945812 |
79 |
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia. |
Convergence Pharmaceuticals |
32452679 |
53 |
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Haisco Pharmaceutical Group |
27432763 |
76 |
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators. |
Sumitomo Dainippon Pharma |
30629436 |
66 |
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H |
Suven Life Sciences |
26542964 |
15 |
Synthesis, biological activity evaluation and molecular docking studies of novel coumarin substituted thiazolyl-3-aryl-pyrazole-4-carbaldehydes. |
National Institute of Technology |
30248655 |
64 |
Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity. |
Japan Tobacco |
29138024 |
213 |
(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent. |
De Montfort University |
29116786 |
265 |
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. |
Idorsia Pharmaceuticals |
29995408 |
293 |
Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition. |
Washington State University |
29259755 |
55 |
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. |
Japan Tobacco |
29724589 |
40 |
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism. |
Mitsubishi Tanabe Pharma |
28838696 |
45 |
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators. |
Sumitomo Dainippon Pharma |
29161514 |
7 |
Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a?-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease. |
Medifron Dbt |
28557445 |
11 |
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. |
Bayer |
28537398 |
114 |
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. |
Bristol-Myers Squibb |
25540906 |
83 |
Identification and further development of potent TBK1 inhibitors. |
Technical University of Dortmund |