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QPatch: the missing link between HTS and ion channel drug discovery.
Mathes C, Friis S, Finley M, Liu Y. Mathes C, et al. Comb Chem High Throughput Screen. 2009 Jan;12(1):78-95. doi: 10.2174/138620709787047948. Comb Chem High Throughput Screen. 2009. PMID: 19149494 Review.
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization.
Gopalakrishnan M, Buckner SA, Whiteaker KL, Shieh CC, Molinari EJ, Milicic I, Daza AV, Davis-Taber R, Scott VE, Sellers D, Chess-Williams R, Chapple CR, Liu Y, Liu D, Brioni JD, Sullivan JP, Williams M, Carroll WA, Coghlan MJ. Gopalakrishnan M, et al. J Pharmacol Exp Ther. 2002 Oct;303(1):379-86. doi: 10.1124/jpet.102.034538. J Pharmacol Exp Ther. 2002. PMID: 12235274
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME. Scanio MJ, et al. Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29. Bioorg Med Chem. 2010. PMID: 20965738
Block of Nav1.8 by small molecules.
Krafte DS, Chapman M, Marron B, Atkinson R, Liu Y, Ye F, Curran M, Kort M, Jarvis MF. Krafte DS, et al. Channels (Austin). 2007 May-Jun;1(3):152-3. doi: 10.4161/chan.4760. Epub 2007 Jul 18. Channels (Austin). 2007. PMID: 18690030
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