Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor
Heffron, Timothy P., Berry, Megan, Castanedo, Georgette, Chang, Christine, Chuckowree, Irina, Dotson, Jennafer, Folkes, Adrian, Gunzner, Janet, Lesnick, John D., Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Olivero, Alan, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steve, Sutherlin, Daniel P., Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wong, Susan, Zhu, Bing-yan
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
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GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway
Wallin, Jeffrey J, Edgar, Kyle A, Guan, Jane, Berry, Megan, Prior, Wei Wei, Lee, Leslie, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Olivero, Alan G, Sutherlin, Daniel P, O'Brien, Carol, Spoerke, Jill M, Patel, Sonal, Lensun, Letitia, Kassees, Robert, Ross, Leanne, Lackner, Mark R, Sampath, Deepak, Belvin, Marcia, Friedman, Lori S
Published in Molecular cancer therapeutics (01.12.2011)
Published in Molecular cancer therapeutics (01.12.2011)
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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)
Heffron, Timothy P, Heald, Robert A, Ndubaku, Chudi, Wei, BinQing, Augistin, Martin, Do, Steven, Edgar, Kyle, Eigenbrot, Charles, Friedman, Lori, Gancia, Emanuela, Jackson, Philip S, Jones, Graham, Kolesnikov, Aleksander, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, McLean, Neville, Mörtl, Mario, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Staben, Steven T, Steinbacher, Stefan, Tsui, Vickie, Wallin, Jeffrey, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR
Heffron, Timothy P, Ndubaku, Chudi O, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Drobnick, Joy, Edgar, Kyle, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Plise, Emile G, Sideris, Steve, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin, Olivero, Alan G
Published in ACS medicinal chemistry letters (14.04.2016)
Published in ACS medicinal chemistry letters (14.04.2016)
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The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α
Heffron, Timothy P, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Dotson, Jennafer, Edgar, Kyle, Goldsmith, Richard, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Ndubaku, Chudi, Nonomiya, Jim, Olivero, Alan G, Pang, Jodie, Plise, Emile G, Sideris, Steve, Trapp, Sean, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin
Published in Journal of medicinal chemistry (27.09.2012)
Published in Journal of medicinal chemistry (27.09.2012)
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N-Arylpiperazinyl-N‘-propylamino Derivatives of Heteroaryl Amides as Functional Uroselective α1-Adrenoceptor Antagonists
Elworthy, Todd R, Ford, Anthony P. D. W, Bantle, Gary W, Morgans, David J, Ozer, Rachel S, Palmer, Wylie S, Repke, David B, Romero, Magarita, Sandoval, Leticia, Sjogren, Eric B, Talamás, Francisco X, Vazquez, Alfredo, Wu, Helen, Arredondo, Nicolas F, Blue, David R, DeSousa, Andrea, Gross, Lisa M, Kava, M. Shannon, Lesnick, John D, Vimont, Rachel L, Williams, Timothy J, Zhu, Quan-Ming, Pfister, Jürg R, Clarke, David E
Published in Journal of medicinal chemistry (15.08.1997)
Published in Journal of medicinal chemistry (15.08.1997)
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Human cloned α1A-adrenoceptor isoforms display α1L-adrenoceptor pharmacology in functional studies
Daniels, Donald V., Gever, Joel R., Jasper, Jeffrey R., Kava, M.Shannon, Lesnick, John D., Meloy, Trena D., Stepan, George, Williams, Timothy J., Clarke, David E., Chang, David J., Ford, Anthony P.D.W.
Published in European journal of pharmacology (01.04.1999)
Published in European journal of pharmacology (01.04.1999)
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Journal Article
Ligand Efficacy and Potency at Recombinant α2 Adrenergic Receptors
Jasper, Jeffrey R, Lesnick, John D, Chang, L.Katy, Yamanishi, Susan S, Chang, Thomas K, Hsu, Sherry A.O, Daunt, David A, Bonhaus, Douglas W, Eglen, Richard M
Published in Biochemical pharmacology (01.04.1998)
Published in Biochemical pharmacology (01.04.1998)
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Molecular cloning, genomic characterization and expression of novel human α1A‐adrenoceptor isoforms
Chang, David J, Chang, Thomas K, Yamanishi, Susan S, Salazar, F.H.Rick, Kosaka, Alan H, Khare, Reena, Bhakta, Sunil, Jasper, Jeffrey R, Shieh, Ing-Shih, Lesnick, John D, Ford, Anthony P.D.W, Daniels, Donald V, Eglen, Richard M, Clarke, David E, Bach, Chinh, Chan, Hardy W
Published in FEBS letters (30.01.1998)
Published in FEBS letters (30.01.1998)
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Pharmacological pleiotropism of the human recombinant α1A‐adrenoceptor: implications for α1‐adrenoceptor classification
Ford, Anthony P D W, Daniels, Donald V, Chang, David J, Gever, Joel R, Jasper, Jeffrey R, Lesnick, John D, Clarke, David E
Published in British journal of pharmacology (01.07.1997)
Published in British journal of pharmacology (01.07.1997)
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Pharmacological pleiotropism of the human recombinant α 1A ‐adrenoceptor: implications for α 1 ‐adrenoceptor classification
Ford, Anthony P D W, Daniels, Donald V, Chang, David J, Gever, Joel R, Jasper, Jeffrey R, Lesnick, John D, Clarke, David E
Published in British journal of pharmacology (09.02.2009)
Published in British journal of pharmacology (09.02.2009)
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Ligand Efficacy and Potency at Recombinant α 2 Adrenergic Receptors : Agonist-Mediated [ 35s]gtpγs Binding
Jasper, Jeffrey R, Lesnick, John D, Chang, L.Katy, Yamanishi, Susan S, Chang, Thomas K, Hsu, Sherry A.O, Daunt, David A, Bonhaus, Douglas W, Eglen, Richard M
Published in Biochemical pharmacology (1998)
Published in Biochemical pharmacology (1998)
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Journal Article
Human cloned α 1A-adrenoceptor isoforms display α 1L-adrenoceptor pharmacology in functional studies
Daniels, Donald V., Gever, Joel R., Jasper, Jeffrey R., Kava, M.Shannon, Lesnick, John D., Meloy, Trena D., Stepan, George, Williams, Timothy J., Clarke, David E., Chang, David J., Ford, Anthony P.D.W.
Published in European journal of pharmacology (1999)
Published in European journal of pharmacology (1999)
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Journal Article
Molecular cloning, genomic characterization and expression of novel human α 1A-adrenoceptor isoforms
Chang, David J, Chang, Thomas K, Yamanishi, Susan S, Salazar, F.H.Rick, Kosaka, Alan H, Khare, Reena, Bhakta, Sunil, Jasper, Jeffrey R, Shieh, Ing-Shih, Lesnick, John D, Ford, Anthony P.D.W, Daniels, Donald V, Eglen, Richard M, Clarke, David E, Bach, Chinh, Chan, Hardy W
Published in FEBS letters (30.01.1998)
Published in FEBS letters (30.01.1998)
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Journal Article
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists
Elworthy, T R, Ford, A P, Bantle, G W, Morgans, Jr, D J, Ozer, R S, Palmer, W S, Repke, D B, Romero, M, Sandoval, L, Sjogren, E B, Talamás, F X, Vazquez, A, Wu, H, Arredondo, N F, Blue, Jr, D R, DeSousa, A, Gross, L M, Kava, M S, Lesnick, J D, Vimont, R L, Williams, T J, Zhu, Q M, Pfister, J R, Clarke, D E
Published in Journal of medicinal chemistry (15.08.1997)
Published in Journal of medicinal chemistry (15.08.1997)
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