The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28254166 |
81 |
Discovery of novel BTK inhibitors with carboxylic acids. |
Merck |
| 28523109 |
79 |
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. |
Glaxosmithkline |
| 27939174 |
84 |
Challenges in the development of an M |
Vanderbilt University Medical Center |
| 28105282 |
95 |
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with |
Merck |
| 27839686 |
65 |
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold. |
Merck Research Laboratories |
| 27815121 |
132 |
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects. |
Merck |
| 27994747 |
66 |
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. |
Merck |
| 27579577 |
91 |
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers. |
Actelion Pharmaceuticals |
| 26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
| 26288685 |
59 |
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys. |
Merck Research Laboratories |
| 26231163 |
50 |
Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. |
Actelion Pharmaceuticals |
| 25286150 |
75 |
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists. |
Astrazeneca |
| 26005536 |
92 |
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys. |
Merck Research Laboratories |
| 26005524 |
147 |
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. |
Merck Research Laboratories |
| 22761000 |
123 |
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
Jagiellonian University |
| 25087753 |
240 |
Prediction of Thorough QT study results using action potential simulations based on ion channel screens. |
University of Oxford |
| 21300721 |
90 |
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
University of Oxford |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 25155913 |
32 |
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa. |
Astrazeneca |
| 24754640 |
28 |
New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
Universidad Complutense |
| 24660890 |
12 |
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
Merck |
| 23688558 |
37 |
Antagonism of L-type Ca2+ channels CaV1.3 and CaV1.2 by 1,4-dihydropyrimidines and 4H-pyrans as dihydropyridine mimics. |
Northwestern University |
| 23651412 |
90 |
Structure-activity relationship of N,N'-disubstituted pyrimidinetriones as Ca(V)1.3 calcium channel-selective antagonists for Parkinson's disease. |
Northwestern University |
| 23200256 |
54 |
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor. |
Astrazeneca |
| 23098566 |
17 |
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain. |
Merck Research Laboratories |
| 22364528 |
412 |
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia. |
Merck Research Laboratories |
| 22607672 |
28 |
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
Merck Research Laboratories |
| 19645482 |
245 |
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement. |
Merck Research Laboratories |
| 10956198 |
2 |
Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists. |
State University of New York |
| 8709127 |
29 |
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers. |
Universit£ |
| 7562902 |
114 |
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. |
Smithkline Beecham Pharmaceuticals |
| 7837222 |
14 |
Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 8246246 |
13 |
A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels. |
State University of New York |
| 1377748 |
16 |
Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
Alter |
| 2329573 |
8 |
Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines. |
Squibb Institute For Medical Research |
| 3184128 |
22 |
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity. |
Ortho Pharmaceutical |
| 2435904 |
12 |
Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation. |
TBA |
| 10522703 |
103 |
Design and synthesis of novel dihydropyridine alpha-1a antagonists. |
Synaptic Pharmaceutical |
| 21942426 |
113 |
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders. |
Merck |
| 21621998 |
110 |
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines. |
Merck Frosst Centre For Therapeutic Research |
| 21514824 |
91 |
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists. |
Merck Research Laboratories |
| 21257308 |
28 |
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors. |
Merck Research Laboratories |
| 21316226 |
12 |
Pyridyl amides as potent inhibitors of T-type calcium channels. |
Merck Research Laboratories |
| 20382537 |
138 |
Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
Northwestern University |
| 19888755 |
43 |
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia. |
Wyeth Research |
| 19203272 |
1 |
Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile. |
University of Padova |
| | 3 |
4-Biaryl-substituted dihydropyridines with an unusual antiperiplanar conformation |
TBA |
| | 24 |
Heterocyclic guanidines as calcium antagonists |
TBA |
| 19481932 |
164 |
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors. |
Merck Research Laboratories |
| 18817368 |
57 |
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. |
Merck Research Laboratories |
| 17588748 |
46 |
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. |
Merck Research Laboratories |
| 32248693 |
73 |
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria. |
University of Washington |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 27774123 |
37 |
Discovery of AZD2716: A Novel Secreted Phospholipase A |
Astrazeneca |
| 27437080 |
96 |
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure. |
Merck Research Laboratories |
| 31566384 |
134 |
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against |
Glaxosmithkline |
| 30624919 |
502 |
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
Recordati |
| 10447952 |
16 |
Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships. |
State University of New York |
| 30879840 |
36 |
Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents. |
Astrazeneca |
| 30500190 |
36 |
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model. |
TBA |
| 31385706 |
9 |
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
The Walter and Eliza Hall Institute of Medical Research |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 31487175 |
195 |
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
Merck |
| 9784106 |
22 |
Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones. |
Chugai Pharmaceutical |
| 30613325 |
88 |
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia. |
Merck |
| 30389294 |
112 |
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase. |
Merck |
| 8558529 |
195 |
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
Hoechst-Roussel Pharmaceuticals |
| 8474099 |
3 |
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile. |
Università |
| 24412109 |
18 |
Successful reduction of off-target hERG toxicity by structural modification of a T-type calcium channel blocker. |
The Catholic University of Korea |
| 24063433 |
72 |
Structure-activity relationships and discovery of a G protein biased ? opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
Trevena |
| 7473567 |
7 |
Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity. |
Università |
| 16913709 |
1 |
Calcium channel antagonists discovered by a multidisciplinary approach. |
Universit£ |
| 30429950 |
98 |
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists. |
Merck |
| 30429949 |
59 |
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition. |
Merck |
| 29571157 |
2 |
Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues. |
University of Siena |
| 30034586 |
90 |
Design of Selective sPLA |
Astrazeneca |
| 29116786 |
265 |
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. |
Idorsia Pharmaceuticals |
| 29074257 |
115 |
Discovery and evaluation of Ca |
Idorsia Pharmaceuticals |
| 29066309 |
87 |
Discovery and evaluation of Ca |
Idorsia Pharmaceuticals |
| 29456796 |
51 |
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1. |
Glaxosmithkline |
| 2435903 |
4 |
Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters. |
TBA |
| 2142737 |
14 |
4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies. |
State University of New York |
| 28753313 |
45 |
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid) |
Sage Therapeutics |
| 28431879 |
123 |
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores. |
Merck |
| 15131245 |
86 |
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. |
Sanofi-Synthelabo Recherche |
| 12761331 |
97 |
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. |
Case Western Reserve University |
| 12721338 |
61 |
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. |
Pudue Pharma Discovery Research |
| 12649361 |
779 |
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. |
Case Western Reserve University |
| 12538838 |
14 |
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor. |
Taisho Pharmaceutical |
| 11750180 |
139 |
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. |
Eli Lilly |
| 11438309 |
51 |
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. |
Janssen Research Foundation |
| 11082453 |
77 |
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse. |
Abbott Laboratories |
| 9454810 |
72 |
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. |
Sanofi Recherche |
| 8996185 |
121 |
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. |
SynthÉLabo Recherche |
| 8935801 |
586 |
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
Janssen Research Foundation |
| 8564266 |
77 |
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. |
Vrije Universiteit |
| 7109844 |
11 |
The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats. |
University of Arizona |
| 3012067 |
36 |
(-)-[3H] desmethoxyverapamil labels multiple calcium channel modulator receptors in brain and skeletal muscle membranes: differentiation by temperature and dihydropyridines. |
Johns Hopkins University |
| 2338642 |
17 |
[3H]TA-3090, a selective benzothiazepine-type calcium channel receptor antagonist: in vitro characterization. |
Marion Merrell Dow |
| 1352553 |
38 |
Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. |
University of North Carolina |
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