220 results on '"Sack, John S."'
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2. Discovery of Non-Nucleotide Small-Molecule STING AgonistsviaChemotype Hybridization
3. X-ray structure of a human cardiac muscle troponin C/troponin I chimera in two crystal forms
4. Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists
5. Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies
6. Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists
7. Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists
8. Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists
9. Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis
10. Tricyclic-Carbocyclic RORγt Inverse Agonists—Discovery of BMS-986313
11. Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach
12. Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists
13. X-Ray Crystal Structure of Bone Marrow Kinase in the X Chromosome: A Tec Family Kinase
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 bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
16. Discovery of Non-Nucleotide Small-Molecule STING Agonists viaChemotype Hybridization
17. [9] CHAIN: A crystallographic modeling program
18. Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors
19. Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt—Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy
20. Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists
21. Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis
22. Discovery of highly potent, selective, covalent inhibitors of JAK3
23. Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors
24. Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors
25. Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors
26. 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors
27. Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders
28. Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors
29. The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode
30. Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor
31. Correction to N-(Cycloalkylamino)acyl-2-aminothiazole Inhibitors of Cyclin-Dependent Kinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide (BMS-387032), a Highly Efficacious and Selective Antitumor Agent
32. Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors
33. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms
34. Discovery of pyrrolo[2,1- f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors
35. Pyrrolo[1,2- f]triazines as JAK2 inhibitors: Achieving potency and selectivity for JAK2 over JAK3
36. [13] Preparation of calmodulin crystals
37. Contacts Between Molecular Surfaces in Crystals of Deoxygenated Human Hemoglobins A, C, F, and S
38. 5-Amino-pyrazoles as potent and selective p38α inhibitors
39. Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
40. Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2- f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase
41. Design, synthesis and structure–activity relationships of novel biarylamine-based Met kinase inhibitors
42. Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
43. Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors
44. Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors
45. 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
46. Benzothiazole based inhibitors of p38α MAP kinase
47. Structural basis for CARM1 inhibition by indole and pyrazole inhibitors
48. 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
49. N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation
50. Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily
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