194 results on '"Melancon, Bruce J."'
Search Results
2. mGlu1-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice
3. On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy
4. Editor's Response to a Letter on “3D Printing Has an Imperative Role in Colitis Management” by Sahoo and Singh
5. Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease
6. Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Imaging Applications
7. Forging Ahead with ASSAY
8. Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery
9. Interview with Craig W. Lindsley, PhD
10. Muscarinic Receptors Allosteric Modulation
11. Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Kinase Signaling
12. Call for Special Issue Papers: Special Issue on High-throughput Technologies for the Discovery and Development of Chemical Probes and Pharmacological Tools
13. Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Kinase Signaling
14. Call for Special Issue Papers: Special Issue on High-throughput Technologies for the Discovery and Development of Chemical Probes and Pharmacological Tools
15. Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds
16. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs
17. Inhibition of Histone Deacetylases 1, 2, and 3 Enhances Clearance of Cholesterol Accumulation in Niemann-Pick C1 Fibroblasts
18. 52500 Characterization of a Series of 1,4-diaryl-pyrazolo-pyridinones as Anti-Leishmanial Agents
19. Chromophore formation in resorcinarene solutions and the visual detection of mono- and oligosaccharides
20. SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs
21. VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate
22. 4040 Investigation of a Series of 1,4-diaryl-pyrazolo-pyridinones as Anti-Leishmanial Agents
23. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides
24. 2-Hydroxypropyl-β-cyclodextrin is the active component in a triple combination formulation for treatment of Niemann-Pick C1 disease
25. Development of a target-free high-throughput screening platform for the discovery of antileishmanial compounds
26. The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor
27. Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands
28. Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology
29. Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs
30. Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core
31. Corrigendum to “Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides” [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179–5184]
32. Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1Positive Allosteric Modulators
33. Changes on the Horizon for Drug Repurposing, Rescue, and Repositioning at ASSAY
34. Challenges in the development of an M 4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides
35. Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A
36. Optimization of M 4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology
37. Challenges in the development of an M 4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs
38. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia
39. Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators.
40. Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354
41. Structural basis of allosteric modulation of metabotropic glutamate receptor activation and desensitization
42. Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: The continued optimization of an MLPCN probe molecule
43. Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: Continued optimization of an MLPCN probe molecule
44. Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia
45. Crystal structure of HDAC6: insights into molecular assembly, selective inhibition and microtubule deacetylation
46. Structural insights into HDAC6 tubulin deacetylation and its selective inhibition
47. Discovery and optimization of a novel series of highly CNS penetrant M 4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3- d ]pyrimidine core
48. A concise Diels–Alder strategy leading to congeners of the ABC ring system of the marine alkaloid ‘upenamide
49. Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012
50. Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor
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