192 results on '"Kish, Kevin"'
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2. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors
3. Crystallographic Structures of the Ligand-Binding Domains of the Androgen Receptor and Its T877A Mutant Complexed with the Natural Agonist Dihydrotestosterone
4. Design, Structure–Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors
5. Structure–activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors
6. Structure-Activity Relationship (SAR) Studies on Substituted 2-(Pyridin-2-ylamino)-N-(pyridin-3-yl)isonicotinamide as Highly Potent, Selective and Brain Penetrant Glycogen Synthase Kinase-3 (GSK-3) Inhibitors
7. Dynamically Optimizing Experiment Schedules of a Laboratory Robot System with Simulated Annealing
8. Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor
9. Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs
10. Core Modifications to the 4-(4,4-Dimethylpiperidinyl) 2,6-Dimethylpyridinyl Class of Hiv-1 Allosteric Integrase Inhibitors
11. Improving the diffraction quality of heat‐shock protein 47 crystals.
12. Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors
13. Involvement of DPP-IV catalytic residues in enzyme–saxagliptin complex formation
14. Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats
15. Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
16. 5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors
17. Structure–Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors
18. Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor
19. Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core
20. Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies
21. The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase
22. Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors
23. Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: Observation of extensive dynamics in an enzyme/inhibitor complex
24. The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode
25. Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing
26. Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors
27. Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors
28. 7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
29. Discovery of pyrrolo[2,1- f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors
30. Investigation of the mode of binding of a novel series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides to the hepatitis C virus polymerase
31. Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
32. 5-Amino-pyrazoles as potent and selective p38α inhibitors
33. Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
34. Phenyltriazolinones as potent factor Xa inhibitors
35. The Discovery of Asunaprevir (BMS-650032), An Orally Efficacious NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
36. Aroylguanidine-based factor Xa inhibitors: The discovery of BMS-344577
37. Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors
38. Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778)
39. Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
40. Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors
41. Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors
42. The discovery of ( R)-2-( sec-butylamino)- N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)—A potent and efficacious p38α MAP kinase inhibitor
43. Benzothiazole based inhibitors of p38α MAP kinase
44. Small Molecule Receptor Protein Tyrosine Phosphatase γ (RPTPγ) Ligands That Inhibit Phosphatase Activity via Perturbation of the Tryptophan–Proline–Aspartate (WPD) Loop
45. Corrigendum to “Investigation of the mode of binding of a novel series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides to the hepatitis C virus polymerase” [Bioorg. Med. Chem. Lett. 21 (2011) 2212]
46. Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase γ in three different crystal forms
47. Structural basis for CARM1 inhibition by indole and pyrazole inhibitors
48. Image Annotation and Database Mining to Create a Novel Screen for the Chemotype-Dependent Crystallization of HCV NS3 Protease
49. Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases
50. Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors
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