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Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays.
Kraus RL, Zhao F, Pall PS, Zhou D, Vardigan JD, Danziger A, Li Y, Daley C, Ballard JE, Clements MK, Klein RM, Holahan MA, Greshock TJ, Kim RM, Layton ME, Burgey CS, Serra J, Henze DA, Houghton AK. Kraus RL, et al. Among authors: daley c. Sci Transl Med. 2021 May 19;13(594):eaay1050. doi: 10.1126/scitranslmed.aay1050. Sci Transl Med. 2021. PMID: 34011626
Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.
Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME. Pero JE, et al. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22. Bioorg Med Chem Lett. 2017. PMID: 28465103
Kinetic Analysis of Membrane Potential Dye Response to NaV1.7 Channel Activation Identifies Antagonists with Pharmacological Selectivity against NaV1.5.
Finley M, Cassaday J, Kreamer T, Li X, Solly K, O'Donnell G, Clements M, Converso A, Cook S, Daley C, Kraus R, Lai MT, Layton M, Lemaire W, Staas D, Wang J. Finley M, et al. Among authors: daley c. J Biomol Screen. 2016 Jun;21(5):480-9. doi: 10.1177/1087057116629669. Epub 2016 Feb 9. J Biomol Screen. 2016. PMID: 26861708
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.
Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME. Roecker AJ, et al. Among authors: daley c. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28389149
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ, Layton ME, Pero JE, Kelly MJ 3rd, Greshock TJ, Kraus RL, Li Y, Klein R, Clements M, Daley C, Jovanovska A, Ballard JE, Wang D, Zhao F, Brunskill APJ, Peng X, Wang X, Sun H, Houghton AK, Burgey CS. Roecker AJ, et al. Among authors: daley c. ACS Med Chem Lett. 2021 Jun 1;12(6):1038-1049. doi: 10.1021/acsmedchemlett.1c00218. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141090 Free PMC article.
Pharmacological Characterization of the Novel and Selective α7 Nicotinic Acetylcholine Receptor-Positive Allosteric Modulator BNC375.
Wang X, Daley C, Gakhar V, Lange HS, Vardigan JD, Pearson M, Zhou X, Warren L, Miller CO, Belden M, Harvey AJ, Grishin AA, Coles CJ, O'Connor SM, Thomson F, Duffy JL, Bell IM, Uslaner JM. Wang X, et al. Among authors: daley c. J Pharmacol Exp Ther. 2020 May;373(2):311-324. doi: 10.1124/jpet.119.263483. Epub 2020 Feb 24. J Pharmacol Exp Ther. 2020. PMID: 32094294
Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.
Stachel SJ, Sanders JM, Henze DA, Rudd MT, Su HP, Li Y, Nanda KK, Egbertson MS, Manley PJ, Jones KL, Brnardic EJ, Green A, Grobler JA, Hanney B, Leitl M, Lai MT, Munshi V, Murphy D, Rickert K, Riley D, Krasowska-Zoladek A, Daley C, Zuck P, Kane SA, Bilodeau MT. Stachel SJ, et al. Among authors: daley c. J Med Chem. 2014 Jul 10;57(13):5800-16. doi: 10.1021/jm5006429. Epub 2014 Jun 19. J Med Chem. 2014. PMID: 24914455
435 results