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Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors
by
Burnett, G. Leslie
,
Yang, Yu C.
,
Aggen, James B.
,
Pitzen, Jennifer
,
Gliedt, Micah K.
,
Semko, Chris M.
,
Marquez, Abby
,
Evans, James W.
,
Wang, Gang
,
Won, Walter S.
,
Tomlinson, Aidan C. A.
,
Kiss, Gert
,
Tzitzilonis, Christos
,
Thottumkara, Arun P.
,
Cregg, James
,
Mellem, Kevin T.
,
Choi, Jong S.
,
Lee, Julie C.
,
Zhao, Yongyuan
,
Lee, Bianca J.
,
Meyerowitz, Justin G.
,
Knox, John E.
,
Jiang, Jingjing
,
Wang, Zhican
,
Wildes, David
,
Wang, Zhengping
,
Singh, Mallika
,
Smith, Jacqueline A. M.
,
Gill, Adrian L.
Published in
Journal of medicinal chemistry
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluorome...
by
Probst, Gary
,
Aubele, Danielle L
,
Bowers, Simeon
,
Dressen, Darren
,
Garofalo, Albert W
,
Hom, Roy K
,
Konradi, Andrei W
,
Marugg, Jennifer L
,
Mattson, Matthew N
,
Neitzel, Martin L
,
Semko, Chris M
,
Sham, Hing L
,
Smith, Jenifer
,
Sun, Minghua
,
Truong, Anh P
,
Ye, Xiaocong M
,
Xu, Ying-zi
,
Dappen, Michael S
,
Jagodzinski, Jacek J
,
Keim, Pamela S
,
Peterson, Brian
,
Latimer, Lee H
,
Quincy, David
,
Wu, Jing
,
Goldbach, Erich
,
Ness, Daniel K
,
Quinn, Kevin P
,
Sauer, John-Michael
,
Wong, Karina
,
Zhang, Hongbin
,
Zmolek, Wes
,
Brigham, Elizabeth F
,
Kholodenko, Dora
,
Hu, Kang
,
Kwong, Grace T
,
Lee, Michael
,
Liao, Anna
,
Motter, Ruth N
,
Sacayon, Patricia
,
Santiago, Pamela
,
Willits, Christopher
,
Bard, Frédérique
,
Bova, Michael P
,
Hemphill, Susanna S
,
Nguyen, Lam
,
Ruslim, Lany
,
Tanaka, Kevin
,
Tanaka, Pearl
,
Wallace, William
,
Yednock, Ted A
,
Basi, Guriqbal S
Published in
Journal of medicinal chemistry
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Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors
by
Truong, Anh P.
,
Aubele, Danielle L.
,
Probst, Gary D.
,
Neitzel, Martin L.
,
Semko, Chris M.
,
Bowers, Simeon
,
Dressen, Darren
,
Hom, Roy K.
,
Konradi, Andrei W.
,
Sham, Hing L.
,
Garofalo, Albert W.
,
Keim, Pamela S.
,
Wu, Jing
,
Dappen, Michael S.
,
Wong, Karina
,
Goldbach, Erich
,
Quinn, Kevin P.
,
Sauer, John-Michael
,
Brigham, Elizabeth F.
,
Wallace, William
,
Nguyen, Lan
,
Hemphill, Susanna S.
,
Bova, Michael P.
,
Basi, Guriqbal
Published in
Bioorganic & medicinal chemistry letters
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Design, synthesis and structure–activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors
by
Aubele, Danielle L.
,
Truong, Anh P.
,
Dressen, Darren B.
,
Probst, Gary D.
,
Bowers, Simeon
,
Mattson, Matthew N.
,
Semko, Chris M.
,
Sun, Minghua
,
Garofalo, Albert W.
,
Konradi, Andrei W.
,
Sham, Hing L.
,
Zmolek, Wes
,
Wong, Karina
,
Goldbach, Erich
,
Quinn, Kevin P.
,
Sauer, John-Michael
,
Brigham, Elizabeth F.
,
Wallace, William
,
Nguyen, Lan
,
Bova, Michael P.
,
Hemphill, Susanna S.
,
Basi, Guriqbal
Published in
Bioorganic & medicinal chemistry letters
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II)
by
Ye, Xiaocong M.
,
Konradi, Andrei W.
,
Smith, Jenifer
,
Aubele, Danielle L.
,
Garofalo, Albert W.
,
Marugg, Jennifer
,
Neitzel, Marty L.
,
Semko, Chris M.
,
Sham, Hing L.
,
Sun, Minghua
,
Truong, Anh P.
,
Wu, Jing
,
Zhang, Hongbin
,
Goldbach, Erich
,
Sauer, John-Michael
,
Brigham, Elizabeth F.
,
Bova, Michael
,
Basi, Guriqbal S.
Published in
Bioorganic & medicinal chemistry letters
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Abstract 4877: Allosteric inhibition of SHP2 variants containing cancer-associated activating mutations
by
Wildes, David
,
Aay, Naing
,
Buckl, Andreas
,
Hsieh, Daphne
,
Jogalekar, Ashutosh S.
,
Kiss, Gert
,
Koltun, Elena S.
,
Marquez, Abby
,
Mellem, Kevin T.
,
Romero, Jason
,
Saldajeno-Concar, Mae
,
Schulze, Christopher J.
,
Semko, Chris M.
,
Won, Walter
,
Nichols, Robert J.
,
Stahlhut, Carlos
,
Tzitzilonis, Christos
,
Gill, Adrian L.
,
Smith, Jacqueline A.
Published in
Cancer research (Chicago, Ill.)
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Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity
by
Koltun, Elena S.
,
Aay, Naing
,
Buckl, Andreas
,
Jogalekar, Ashutosh S.
,
Kiss, Gert
,
Marquez, Abby
,
Mellem, Kevin T.
,
Mordec, Kasia
,
Saldajeno-Concar, Mae
,
Semko, Chris M.
,
Tibrewal, Nidhi
,
Tzitzilonis, Christos
,
Won, Walter
,
Smith, Jacqueline A.
,
Wilson, Susan E.
,
Nichols, Robert J.
,
Wang, Zhengping
,
Wilds, David
,
Singh, Mallika
,
Gill, Adrian L.
Published in
Cancer research (Chicago, Ill.)
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8
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Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(tri...
by
Probst, Gary
,
Aubele, Danielle L.
,
Bowers, Simeon
,
Dressen, Darren
,
Garofalo, Albert W.
,
Hom, Roy K.
,
Konradi, Andrei W.
,
Marugg, Jennifer L.
,
Mattson, Matthew N.
,
Neitzel, Martin L.
,
Semko, Chris M.
,
Sham, Hing L.
,
Smith, Jenifer
,
Sun, Minghua
,
Truong, Anh P.
,
Ye, Xiaocong M.
,
Xu, Ying-zi
,
Dappen, Michael S.
,
Jagodzinski, Jacek J.
,
Keim, Pamela S.
,
Peterson, Brian
,
Latimer, Lee H.
,
Quincy, David
,
Wu, Jing
,
Goldbach, Erich
,
Ness, Daniel K.
,
Quinn, Kevin P.
,
Sauer, John-Michael
,
Wong, Karina
,
Zhang, Hongbin
,
Zmolek, Wes
,
Brigham, Elizabeth F.
,
Kholodenko, Dora
,
Hu, Kang
,
Kwong, Grace T.
,
Lee, Michael
,
Liao, Anna
,
Motter, Ruth N.
,
Sacayon, Patricia
,
Santiago, Pamela
,
Willits, Christopher
,
Bard, Frédérique
,
Bova, Michael P.
,
Hemphill, Susanna S.
,
Nguyen, Lam
,
Ruslim, Lany
,
Tanaka, Kevin
,
Tanaka, Pearl
,
Wallace, William
,
Yednock, Ted A.
,
Basi, Guriqbal S.
Published in
Journal of medicinal chemistry
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A Label-Free Approach to Identify Inhibitors of α4β7-Mediated Cell Adhesion to MadCAM
by
Bova, Michael P.
,
Nguyen, Lan
,
Wallace, William
,
Garrido, Caroline
,
Xu, Ying-Zi
,
Semko, Chris
,
Cockcroft, Kelly
,
Sandberg, Eric
,
Bard, Frederique
Published in
SLAS discovery
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Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent [gamma]-secretase inhibitors
by
Aubele, Danielle L
,
Truong, Anh P
,
Dressen, Darren B
,
Probst, Gary D
,
Bowers, Simeon
,
Mattson, Matthew N
,
Semko, Chris M
,
Sun, Minghua
,
Garofalo, Albert W
,
Konradi, Andrei W
,
Sham, Hing L
,
Zmolek, Wes
,
Wong, Karina
,
Goldbach, Erich
,
Quinn, Kevin P
,
Sauer, John-Michael
,
Brigham, Elizabeth F
,
Wallace, William
,
Nguyen, Lan
,
Bova, Michael P
,
Hemphill, Susanna S
,
Basi, Guriqbal
Published in
Bioorganic & medicinal chemistry letters
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Corrigendum to “Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors” [Bioorg. Med....
by
Truong, Anh P.
,
Aubele, Danielle L.
,
Probst, Gary D.
,
Neitzel, Martin L.
,
Semko, Chris M.
,
Bowers, Simeon
,
Dressen, Darren
,
Hom, Roy K.
,
Konradi, Andrei W.
,
Sham, Hing L.
,
Garofalo, Albert W.
,
Keim, Pamela S.
,
Wu, Jing
,
Dappen, Michael S.
,
Wong, Karina
,
Goldbach, Erich
,
Quinn, Kevin P.
,
Sauer, John-Michael
,
Brigham, Elizabeth F.
,
Wallace, William
,
Nguyen, Lan
,
Hemphill, Susanna S.
,
Bova, Michael P.
,
Bard, Frédérique
,
Yednock, Ted A.
,
Basi, Guriqbal
Published in
Bioorganic & medicinal chemistry letters
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Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline g-secretase inhibitors
by
Truong, Anh P
,
Aubele, Danielle L
,
Probst, Gary D
,
Neitzel, Martin L
,
Semko, Chris M
,
Bowers, Simeon
,
Dressen, Darren
,
Hom, Roy K
,
Konradi, Andrei W
,
Sham, Hing L
,
Garofalo, Albert W
,
Keim, Pamela S
,
Wu, Jing
,
Dappen, Michael S
,
Wong, Karina
,
Goldbach, Erich
,
Quinn, Kevin P
,
Sauer, John-Michael
,
Brigham, Elizabeth F
,
Wallace, William
,
Nguyen, Lan
,
Hemphill, Susanna S
,
Bova, Michael P
,
Basi, Guriqbal
Published in
Bioorganic & medicinal chemistry letters
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Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline y-secretase inhibitors
by
TRUONG, Anh P
,
AUBELE, Danielle L
,
GAROFALO, Albert W
,
KEIM, Pamela S
,
JING WU
,
DAPPEN, Michael S
,
WONG, Marina
,
GOLDBACH, Erich
,
QUINN, Kevin P
,
SAUER, John-Michael
,
BRIGHAM, Elizabeth F
,
WALLACE, William
,
PROBST, Gary D
,
NGUYEN, Lan
,
HEMPHILL, Susanna S
,
BOVA, Michael P
,
BASI, Guriqbal
,
NEITZEL, Martin L
,
SEMKO, Chris M
,
BOWERS, Simeon
,
DRESSEN, Darren
,
HOM, Roy K
,
KONRADI, Andrei W
,
SHAM, Hing L
Published in
Bioorganic & medicinal chemistry letters
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Arylsulfonamide pyrimidines as VLA-4 antagonists
by
Xu, Ying-zi
,
Konradi, Andrei W.
,
Bard, Frederique
,
Dappen, Michael
,
Dofiles, Lilibeth
,
Dreyer, Mark
,
Gallager, Ian
,
Garrido, Caroline
,
Krimm, Mike
,
Liao, Zhenmei
,
Messersmith, Elizabeth
,
Mutter, Linda
,
Pleiss, Michael A.
,
Samant, Bhushan
,
Semko, Christopher M.
,
Smith, Jennifer
,
Stappenbeck, Frank
,
Stupi, Brian
,
Vandervert, Chris
,
Welch, Brent
,
Wipke, Brian
,
Yednock, Ted
Published in
Bioorganic & medicinal chemistry letters
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