FDSS7000EX는 Fluorescence 및 Luminescence의 측정이 가능한 high-end 모델로 multiple washing과 같은 다양한 기능이 탑재되어 있습니다.
다양한 suspended/adherent 세포의 움직임을 실시간으로 관찰하여 분석할 수 있습니다. FRET, robot connection등의 다양한 부품들이 옵션으로 장착 가능합니다.

Applications

Hardware

Software

Configuration

Specifications

Type number	FDSS7000EX
Main unit dimensions	Approx. 1500 mm (W)×1030 mm (D)×1450 mm (H)
Main unit	Up to approx. 300 kg
Data analysis system dimensions	600 mm (W)×700 mm (D)×1500 mm (H)
Data analysis system weight	Approx. 50 kg
Pump unit/Tank dimensions	500 mm (W)×500 mm (D)×1200 mm (H)
Pump unit/Tank weight	Approx. 50 kg

Related information

• FDSS Application Note No.1 Chloride ion sensitive fluorescent dye for Drug Screening [0.1MB/PDF]
• FDSS Application Note No.2 CoroNa Red as a potential probe for intracellular sodium imaging [0.1MB/PDF]
• FDSS Application Note No.3 FRET-based Voltage Sensor dyes for Drug Screening [0.1MB/PDF]
• FDSS Application Note No.4 FDSS Cell dispensing unit for Aequorin Flash luminescence [0.4MB/PDF]
• FDSS Application Note No.5 COX flash luminescence screening [0.1MB/PDF]
• FDSS Application Note No.6 Direct comparison of Fast response and Slow response Membrane potential dye using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.7 Multiplexing Calcium Mobilization and Membrane Potential Assays Using the FDSS6000 [0.3MB/PDF]
• FDSS Application Note No.8 Comparison of No Wash Reagent Kits on the FDSS6000 [0.4MB/PDF]
• FDSS Application Note No.9 Effect of Plate Mixing, Fluid Addition Height and Speed on Reducing Addition Artifacts and Negative Control Drift Using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.10 Comparison of Orthogonal Technologies to Confirm Agonist Hits Generated Using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.11 Detection and Modulation of Cardiomyocyte Calcium Oscillations Using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.12 Fluorescence Quenching in Cell-Based Assays Can Be Dye Specific: A Case Study Using Both Fura-2 AM and Fluo-4 AM Calcium Reporter Dyes Using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.13 Incorporating Cell Viability Assays into High Throughput Screening Using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.14 Evaluation of a new intracellular calcium fluorescent reagent using the FDSS6000 [0.4MB/PDF]
• FDSS Application Note No.15 Exposing cells to a single pulse of light of user-defined wavelength and duration using the FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.16 FluxORTM Differentially Identifies K+ Channel Antagonists Using FDSS6000 [0.1MB/PDF]
• FDSS Application Note No.17 Use of Ca2+ oscillations in primary neuron culture: a new HTS model for neuronal diseases [0.3MB/PDF]
• FDSS Application Note No.18 β-arrestin recruitment for GPCR Screening [0.1MB/PDF]
• FDSS Application Note No.19 Fast kinetics enzyme assay High-throughput screening of prolyl isomerase inhibitors [0.1MB/PDF]
• FDSS Application Note No.20 New Tools for Drug Discovery: Multiplexing the monitoring of Ca2+ and cAMP signaling in primary cells using the FDSS/μCell. [0.4MB/PDF]
• FDSS Application Note No.21 Cell-based fluorescent assay for selectivity evaluation between two Na+ channels subtypes [0.2MB/PDF]
• FDSS Application Note No.22 High Speed Data Acquisition Option for FDSS series [0.4MB/PDF]
• FDSS Application Note No.23 BRET1-assay using the FDSS/μCELL imaging plate reader [0.1MB/PDF]
• FDSS Application Note No.24 Evaluation of membrane potential assay kit using the FDSS/μCELL imaging plate reader: Detection ion channel in nicotinic acetylcholine receptors (nAChRs) [0.1MB/PDF]
• FDSS Application Note No.25 Identification of small molecule modulators of reactive oxygen release in TNF-α primed primary human neutrophils. [0.1MB/PDF]
• FDSS Option 1: 1536-Well Format Option with Disposable Tips and Pin Tool Head [0.2MB/PDF]
• FDSS Option 2: High Speed Acquisition Option [0.2MB/PDF]

Publications

Please select a title to view a complete citation via pubmed and web-based resources.

2014

• Anke Bill, Elizabeth M. Rosethorne, Toby C. Kent, Lindsay Fawcett, Lynn Burchell, Michiel T. van Diepen, Anthony Marelli, Sergey Batalov, Loren Miraglia, Anthony P. Orth, Nicole A. Renaud, Steven J. Charlton, Martin Gosling, L. Alex Gaither, Paul J. Groot-Kormelink High Throughput Mutagenesis for Identification of Residues Regulating Human Prostacyclin (hIP) Receptor Expression and Function PLoS One. 2014 Jun 2;9(6):e97973. doi: 10.1371/journal.pone.0097973. eCollection 2014.
• Anke Bill, M. Oana Popa, Michiel T. van Diepen, Abraham Gutierrez, Sarah Lilley, Maria Velkova, Kathryn Acheson, Hedaythul Choudhury, Nicole A. Renaud, Douglas S. Auld, Martin Gosling, Paul J. Groot-Kormelink, L. Alex Gaither Variomics Screen Identifies the Re-entrant Loop of the Calcium-activated Chloride Channel ANO1 That Facilitates Channel Activation J Biol Chem. 2015 Jan 9;290(2):889-903. doi: 10.1074/jbc.M114.618140. Epub 2014 Nov 25.
• Ann-Beth Nørholm, Pierre Francotte, Eric Goffin, Iuliana Botez, Laurence Danober, Pierre Lestage, Bernard Pirotte, Jette S. Kastrup, Lars Olsen, Chris Oostenbrink Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces J Chem Inf Model. 2014 Dec 22;54(12):3404-16. doi: 10.1021/ci500559b. Epub 2014 Dec 9.
• Anuradha Roy High Throughput Screening Operations at the University of Kansas Comb Chem High Throughput Screen. 2014 May;17(4):387-93.
• Bin Cai, Xia Chen, Fang Liu, Jun Li, Lijuan Gu, Jason R. Liu, Jay Liu A Cell-Based Functional Assay Using a Green Fluorescent Protein-Based Calcium Indicator dCys-GCaMP Assay Drug Dev Technol. 2014 Aug;12(6):342-51. doi: 10.1089/adt.2014.584. Epub 2014 Aug 8.
• Cheryse A. Furman, Rebecca A. Roof, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, R. Benjamin Free, Ashwini K. Banala, Noel M. Paul, Vivek Kumar, Christopher D. Sibley, Amy Hauck Newman, David R. Sibley Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists Eur Neuropsychopharmacol. 2014 Nov 29. pii: S0924-977X(14)00324-1. doi: 10.1016/j.euroneuro.2014.11.013. [Epub ahead of print]
• Eunan Hendron, Xizhuo Wang, Yandong Zhou, Xiangyu Cai, Jun-Ichi Goto, Katsuhiko Mikoshiba, Yoshihiro Baba, Tomohiro Kurosaki, Youjun Wang, Donald L. Gill Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs Cell Calcium. 2014 Oct 23;56(6):482-492. doi: 10.1016/j.ceca.2014.10.005. [Epub ahead of print]
Frederic Bassilana, Adam Carlson, Jennifer A DaSilva, Bianka Grosshans, Solange Vidal, Valerie Beck, Barbara Wilmeringwetter, Luis A Llamas, Todd B Showalter, Pascal Rigollier, Aaron Bourret, Arun Ramamurthy, Xu Wu, Fred Harbinski, Samantha Plonsky, Lac Lee, Heinz Ruffner, Paola Grandi, Markus Schirle, Jeremy Jenkins, Andreas W Sailer, Tewis Bouwmeester, Jeffrey A Porter, Vic Myer, Peter M Finan et al. Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39 Nat Chem Biol. 2014 May;10(5):343-9. doi: 10.1038/nchembio.1481. Epub 2014 Mar 16.
• Hongkang Zhang, Beiyan Zou, Fang Du, Kaiping Xu, and Min Li Reporting Sodium Channel Activity Using Calcium Flux: Pharmacological Promiscuity of Cardiac Nav1.5 Mol Pharmacol. 2015 Feb;87(2):207-17. doi: 10.1124/mol.114.094789. Epub 2014 Nov 24.
• Hyekyung P. Cho, Darren W. Engers, Daryl F. Venable, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Kyle A. Emmitte, Alice L. Rodriguez A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity between the Rat and Human Receptors ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15.
• Hyekyung P. Cho, Pedro M. Garcia-Barrantes, John T. Brogan, Corey R. Hopkins, Colleen M. Niswender, Alice L. Rodriguez, Daryl F. Venable, Ryan D. Morrison, Michael Bubser, J. Scott Daniels, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics ACS Chem Biol. 2014 Oct 17;9(10):2334-46. doi: 10.1021/cb500560h. Epub 2014 Aug 28.
• J. Kyle Bruner, Beiyan Zou, Hongkang Zhang, Yixin Zhang, Katharina Schmidt, Min Li Identification of novel small molecule modulators of K2P18.1 two-pore potassium channel Eur J Pharmacol. 2014 Oct 5;740:603-10. doi: 10.1016/j.ejphar.2014.06.021. Epub 2014 Jun 24.
• Jesse E. Hanson, William J. Meilandt, Alvin Gogineni, Paul Reynen, James Herrington, Robby M. Weimer, Kimberly Scearce-Levie, Qiang Zhou Chronic GluN2B Antagonism Disrupts Behavior in Wild-Type Mice Without Protecting Against Synapse Loss or Memory Impairment in Alzheimer's Disease Mouse Models J Neurosci. 2014 Jun 11;34(24):8277-88. doi: 10.1523/JNEUROSCI.5106-13.2014.
• John W. Kehoe, Brian Whitaker, Deidra Bethea, Eilyn R. Lacy, Ken Boakye, Sandra Santulli-Marotto, Mary H. Ryan, Yiqing Feng, John C. Wheeler Isolation and optimization for affinity and biophysical characteristics of anti-CCL17 antibodies from the VH1-69 germline gene Protein Eng Des Sel. 2014 Jun;27(6):199-206. doi: 10.1093/protein/gzu012. Epub 2014 Apr 16.
Julie A. Meade, R. Benjamin Free, Nicole R. Miller, Lani S. Chun, Trevor B. Doyle, Amy E. Moritz, Jennie L. Conroy, Val J. Watts, David R. Sibley (-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling Psychopharmacology (Berl). 2014 Sep 18. [Epub ahead of print]
Junki Miyamoto, Taichi Mizukure, Si-Bum Park, Shigenobu Kishino, Ikuo Kimura, Kanako Hirano, Paolo Bergamo, Mauro Rossi, Takuya Suzuki, Makoto Arita, Jun Ogawa, Soichi Tanabe A gut microbial metabolite of linoleic acid, 10-hydroxy-cis-12-octadecenoic acid, ameliorates intestinal epithelial barrier impairment partially via GPR40/MEK-ERK pathway J Biol Chem. 2014 Dec 10. pii: jbc.M114.610733. [Epub ahead of print]
• Katie L Strong, Yao Jing, Anthony R Prosser, Stephen F Traynelis, Dennis C Liotta NMDA receptor modulators: an updated patent review (2013 – 2014) Expert Opin Ther Pat. 2014 Dec;24(12):1349-66. doi: 10.1517/13543776.2014.972938. Epub 2014 Oct 29.
• Kazuaki Ohara, Takafumi Fukuda, Hiroyuki Okada, Sayoko Kitao, Yuko Ishida, Kyoko Kato, Chika Takahashi, Mikio Katayama, Kunitoshi Uchida, Makoto Tominaga Identification of Significant Amino Acids in Multiple Transmembrane Domains of Human Transient Receptor Potential Ankyrin 1 (TRPA1) for Activation by Eudesmol, an Oxygenized Sesquiterpene in Hop Essential Oil J Biol Chem. 2014 Dec 18. pii: jbc.M114.600932. [Epub ahead of print]
• Kazuyuki Fukushima, Yoshikuni Tabata, Yoichi Imaizumi, Naohiro Kohmura, Michiko Sugawara, Kohei Sawada, Kazuto Yamazaki, Masashi Ito Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors J Biomol Screen. 2014 Jun 30;19(8):1174-1184. [Epub ahead of print]
• Laykea Tafesse, Toshiyuki Kanemasa, Noriyuki Kurose, Jianming Yu, Toshiyuki Asaki, Gang Wu, Yuka Iwamoto, Yoshitaka Yamaguchi, Chiyou Ni, John Engel, Naoki Tsuno, Aniket Patel, Xiaoming Zhou, Takuya Shintani, Kevin Brown, Tsuyoshi Hasegawa, Manjunath Shet, Yasuyoshi Iso, Akira Kato, Donald J. Kyle Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management J Med Chem. 2014 Aug 14;57(15):6781-94. doi: 10.1021/jm500818a. Epub 2014 Aug 1.
• Lindsey C. Morris, Emily L. Days, Maxine Turney, Dehui Mi, Craig W. Lindsley, C. David Weaver, Kevin D. Niswender A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors J Biomol Screen. 2014 Feb 13;19(6):847-858. [Epub ahead of print]
• Matthew F. Rouhier, Rene Raphemot, Jerod S. Denton, Peter M. Piermarini Pharmacological Validation of an Inward-Rectifier Potassium (Kir) Channel as an Insecticide Target in the Yellow Fever MosquitoAedes aegypti PLoS One. 2014 Jun 24;9(6):e100700. doi: 10.1371/journal.pone.0100700. eCollection 2014.
• Michael P. Winters, Nalin Subasinghe, Mark Wall, Edward Beck, Michael R. Brandt, Michael F.A. Finley, Yi Liu, Mary Lou Lubin, Michael P. Neeper, Ning Qin, Christopher M. Flores, Zhihua Sui Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel Bioorg Med Chem Lett. 2014 May 1;24(9):2053-6. doi: 10.1016/j.bmcl.2014.03.062. Epub 2014 Mar 27.
• Mikkel A. Rasmussen, Bjørn Holst, Zeynep Tümer, Mads G. Johnsen, Shuling Zhou, Tina C. Stummann, Poul Hyttel, Christian Clausen Transient p53 Suppression Increases Reprogramming of Human Fibroblasts without Affecting Apoptosis and DNA Damage Stem Cell Reports. 2014 Sep 9;3(3):404-13. doi: 10.1016/j.stemcr.2014.07.006. Epub 2014 Aug 21.
• Mingfei Ji, Xubo Su, Xiaohong Su, Yingyi Chen, Wenkang Huang, Jian Zhang, Zhaobin Gao, Chuangang Li, Xuefeng Lu Identification of Novel Compounds for Human Bitter Taste Receptors Chem Biol Drug Des. 2014 Jul;84(1):63-74. doi: 10.1111/cbdd.12293. Epub 2014 Feb 28.
• Nidhi Jalan-Sakrikar, Julie R. Field, Rebecca Klar, Margrith E. Mattmann, Karen J. Gregory, Rocio Zamorano, Darren W. Engers, Sean R. Bollinger, C. David Weaver, Emily L. Days, L. Michelle Lewis, Thomas J. Utley, Miguel Hurtado, Delphine Rigault, Francine Acher, Adam G. Walker, Bruce J. Melancon, Michael R. Wood, Craig W. Lindsley, P. Jeffrey Conn, Zixiu Xiang, Corey R. Hopkins, and Colleen M. Niswender Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7 ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9.
• R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andrés E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan A. Javitch, Thijs Beuming, Lei Shi, Noel T. Southall, Juan J. Marugan, David R. Sibley Discovery and Characterization of a G Protein–Biased Agonist That Inhibits β-Arrestin Recruitment to the D2 Dopamine Receptor Mol Pharmacol. 2014 Jul;86(1):96-105. doi: 10.1124/mol.113.090563. Epub 2014 Apr 22.
• Rene Raphemot, Matthew F. Rouhier, Daniel R. Swale, Emily Days, C. David Weaver, Kimberly M. Lovell, Leah C. Konkel, Darren W. Engers, Sean F. Bollinger, Corey Hopkins, Peter M. Piermarini , Jerod S. Denton Discovery and Characterization of a Potent and Selective Inhibitor of Aedes aegypti Inward Rectifier Potassium Channels PLoS One. 2014 Nov 6;9(11):e110772. doi: 10.1371/journal.pone.0110772. eCollection 2014.
• Wendy J. Winchester, Katrina Gore, Sophie Glatt, Wendy Petit, Jennifer C. Gardiner, Kelly Conlon, Michael Postlethwaite, Pierre-Philippe Saintot, Sonia Roberts, James R. Gosset, Tomomi Matsuura, Mark D. Andrews, Paul A. Glossop, Michael J. Palmer, Nicola Clear, Susie Collins, Kevin Beaumont, David S. Reynolds Inhibition of TRPM8 Channels Reduces Pain in the Cold Pressor Test in Humans J Pharmacol Exp Ther. 2014 Nov;351(2):259-69. doi: 10.1124/jpet.114.216010. Epub 2014 Aug 14.
• Zhiqiang Wang, Shimeng Liu, Miyo Kakizaki, Yuuki Hirose, Yukiko Ishikawa, Hiromasa Funato, Masashi Yanagisawa, Yonghao Yu, Qinghua Liu Orexin/Hypocretin Activates mTOR Complex 1 (mTORC1) via an Erk/Akt-independent and Calcium-stimulated Lysosome v-ATPase Pathway J Biol Chem. 2014 Nov 14;289(46):31950-9. doi: 10.1074/jbc.M114.600015. Epub 2014 Oct 2.

2013

• Andrew J. Storaska, Jian P. Mei, Meng Wu, Min Li, Susan M. Wade, Levi L. Blazer, Benita Sjögren, Corey R. Hopkins, Craig W. Lindsley, Zhihong Lin, Joseph J. Babcock, Owen McManus, Richard R. Neubig Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay Cell Signal. 2013 Dec;25(12):2848-55. doi: 10.1016/j.cellsig.2013.09.007. Epub 2013 Sep 14.
• C Brenneis, K Kistner, M Puopolo, S Jo, DP Roberson, M Sisignano, D Segal, E J Cobos, B J Wainger, S Labocha, N Ferreirós, C von Hehn, J Tran, G Geisslinger, P W Reeh, B P Bean, C J Woolf Bupivacaine-induced cellular entry of QX-314 and its contribution to differential nerve block Br J Pharmacol. 2014 Jan;171(2):438-51. doi: 10.1111/bph.12466.
• Erica VanderPorten, Lauren Frick, Rebecca Turincio, Peter Thana, William LaMarr, Yichin Liu Label-free high-throughput assays to screen and characterize novel lactate dehydrogenase inhibitors Anal Biochem. 2013 Oct 15;441(2):115-22. doi: 10.1016/j.ab.2013.07.003. Epub 2013 Jul 16.
• Florian P. M. Kohn High Throughput Fluorescent Screening of Membrane Potential and Intracellular Calcium Concentration Under Variable Gravity Conditions Microgravity Sci. Technol. 2013 April, Volume 25, Issue 2, pp 113-120. doi: 10.1007/s12217-012-9331-8
• Hilde Lavreysen, Xavier Langlois, Abdel Ahnaou, Wilhelmus Drinkenburg, Paula te Riele, Ilse Biesmans, Ilse Van der Linden, Luc Peeters, Anton Megens, Cindy Wintmolders, Jose Maria Cid, Andrés A. Trabanco, Jose Ignacio Andrés, Frank M. Dautzenberg, Robert Lütjens, Gregor Macdonald, John R. Atack Pharmacological Characterization of JNJ-40068782, a New Potent, Selective, and Systemically Active Positive Allosteric Modulator of the mGlu2 Receptor and Its Radioligand [3H]JNJ-40068782 J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. doi: 10.1124/jpet.113.204990. Epub 2013 Jun 13.
• Jason T. Manka, Alice L. Rodriguez, Ryan D. Morrison, Daryl F. Venable, Hyekyung P. Cho, Anna L. Blobaum, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23.
• Kentaro Ozawa, Akira T. Komatsubara, Yuhei Nishimura, Tomoyo Sawada, Hiroto Kawafune, Hiroki Tsumoto, Yuichi Tsuji, Jing Zhao, Yoji Kyotani, Toshio Tanaka, Ryosuke Takahashi, Masanori Yoshizumi S-nitrosylation regulates mitochondrial quality control via activation of parkin Sci Rep. 2013;3:2202. doi: 10.1038/srep02202.
• Kentaro Takai, Yasunao Inoue, Yasuko Konishi, Atsushi Suwa, Yoshiharu Uruno, Harumi Matsuda, Tomokazu Nakako, Mutsuko Sakai, Hiroyuki Nishikawa, Gakuji Hashimoto, Takeshi Enomoto, Atsushi Kitamura, Yasuaki Uematsu, Akihiko Kiyoshi, Takaaki Sumiyoshi Identification of N-substituted 8-azatetrahydroquinolone derivatives as selective and orally active M1 and M4 muscarinic acetylcholine receptors agonists Bioorg Med Chem Lett. 2013 Aug 15;23(16):4644-7. doi: 10.1016/j.bmcl.2013.06.013. Epub 2013 Jun 13.
• Kimberly M. Lovell, Andrew S. Felts, Alice L. Rodriguez, Daryl F. Venable, Hyekyung P. Cho, Ryan D. Morrison, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17.
• Lani S. Chun, R. Benjamin Free, Trevor B. Doyle, Xi-Ping Huang, Michele L. Rankin, David R. Sibley D1-D2 Dopamine Receptor Synergy Promotes Calcium Signaling via Multiple Mechanisms Mol Pharmacol. 2013 Aug;84(2):190-200. doi: 10.1124/mol.113.085175. Epub 2013 May 16.
• Mamoru Tasakia, Miki Kobayashi, Yoshiyuki Tenda, Susumu Tsujimoto, Shoko Nakazato, Mako Numazaki, Yasuno Hirano, Hiroshi Matsuda, Tadashi Terasaka, Yasuhiro Miyao, Yasuaki Shimizu, Yoshitaka Hirayama Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of “chemoattractant receptor homologous molecule expressed on Th2 cells” (CRTH2) Eur J Pharm Sci. 2013 Jun 14;49(3):434-40. doi: 10.1016/j.ejps.2013.04.017. Epub 2013 Apr 24.
• Paul H. Tewson, Anne Marie Quinn, Thomas E. Hughes A Multiplexed Fluorescent Assay for Independent Second-Messenger SystemsDecoding GPCR Activation in Living Cells J Biomol Screen. 2013 Aug;18(7):797-806. doi: 10.1177/1087057113485427. Epub 2013 Apr 11.
• Rene Raphemot, C. David Weaver, Jerod S. Denton High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels J Vis Exp. 2013 Jan 27;(71). pii: 4209. doi: 10.3791/4209.
• Rene Raphemot, Matthew F. Rouhier, Rocco D. Gogliotti, Kimberly M. Lovell, Rebecca M. Hine, Dhairyasheel Ghosalkar, Anthony Longo, Klaus W. Beyenbach, Jerod S. Denton, Peter M. Piermarini Eliciting Renal Failure in Mosquitoes with a Small-Molecule Inhibitor of Inward-Rectifying Potassium Channels PLoS One. 2013 May 29;8(5):e64905. doi: 10.1371/journal.pone.0064905. Print 2013.
• Samarjit Patnaik, Juan J. Marugan, Ke Liu, Wei Zheng, Noel Southall, Seameen J. Dehdashti, Annika Thorsell, Markus Heilig, Lauren Bell, Michelle Zook, Bob Eskay, Kyle R. Brimacombe, Christopher P. Austin Structure–Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11.
• Sandra Santulli-Marotto, Jamie Fisher, Theodore Petley, Ken Boakye, Tadas Panavas, Jennifer Luongo, Karl Kavalkovich, Michael Rycyzyn, Bingyuan Wu, Lester Gutshall, Ana Coelho, Cory M. Hogaboam, Mary Ryan Surrogate Antibodies That Specifically Bind and Neutralize CCL17 But Not CCL22 Monoclon Antib Immunodiagn Immunother. 2013 Jun;32(3):162-71. doi: 10.1089/mab.2012.0112.
• Sandra Santulli-Marotto, Ken Boakye, Eilyn Lacy, Sheng-Jiun Wu, Jennifer Luongo, Karl Kavalkovich, Ana Coelho, Cory M. Hogaboam, Mary Ryan Engagement of Two Distinct Binding Domains on CCL17 Is Required for Signaling through CCR4 and Establishment of Localized Inflammatory Conditions in the Lung PLoS One. 2013 Dec 5;8(12):e81465. doi: 10.1371/journal.pone.0081465. eCollection 2013.
• Sebastien Hannedouche, Valerie Beck, Juliet Leighton-Davies, Martin Beibel, Guglielmo Roma, Edward J. Oakeley, Vincent Lannoy, Jerome Bernard, Jacques Hamon, Samuel Barbieri, Inga Preuss, Marie-Christine Lasbennes, Andreas W. Sailer, Thomas Suply, Klaus Seuwen, Christian N. Parker, Frederic Bassilana Identification of the C3a Receptor (C3AR1) as the Target of the VGF-derived Peptide TLQP-21 in Rodent Cells J Biol Chem. 2013 Sep 20;288(38):27434-43. doi: 10.1074/jbc.M113.497214. Epub 2013 Aug 12.
• Shoichiro Ozaki, Akinobu Z. Suzuki, Peter O. Bauer, Etsuko Ebisui, Katsuhiko Mikoshiba 2-Aminoethyl diphenylborinate (2-APB) analogues: Regulation of Ca2+ signaling Biochem Biophys Res Commun. 2013 Nov 15;441(2):286-90. doi: 10.1016/j.bbrc.2013.08.102. Epub 2013 Sep 11.
• Summer E. Young, Matthew T. Duvernay, Michael L. Schulte, Craig W. Lindsley, Heidi E. Hamm Synthesis of Indole Derived Protease-Activated Receptor 4 Antagonists and Characterization in Human Platelets PLoS One. 2013 Jun 11;8(6):e65528. doi: 10.1371/journal.pone.0065528. Print 2013.0
• Susan J. Ramos-Hunter, Darren W. Engers, Kristian Kaufmann, Yu Du, Craig W. Lindsley, C. David Weaver, Gary A. Sulikowski Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18.
• Thomas M. Bridges, Jerri M. Rook, Meredith J. Noetzel, Ryan D. Morrison, Ya Zhou, Rocco D. Gogliotti, Paige N. Vinson, Zixiu Xiang, Carrie K. Jones, Colleen M. Niswender, Craig W. Lindsley, Shaun R. Stauffer, P. Jeffrey Conn, J. Scott Daniels Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizure-Like Adverse Events in Rats Involving a Receptor Agonism-Dependent Mechanism Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.

2012

• Bo-Hye Im, Hyewhon Rhim GABAB receptor-mediated ERK1/2 phosphorylation via a direct interaction with CaV1.3 channels Neurosci Lett. 2012 Mar 28;513(1):89-94. doi: 10.1016/j.neulet.2012.02.014. Epub 2012 Feb 14.
• Caroline Chambon, Claudia Jatzke, Nico Wegener, Andreas Gravius, Wojciech Danysz Using cholinergic M1 receptor positive allosteric modulators to improve memory via enhancement of brain cholinergic communication Eur J Pharmacol. 2012 Dec 15;697(1-3):73-80. doi: 10.1016/j.ejphar.2012.10.011. Epub 2012 Oct 17.
• Christina Mølck, Kasper Harpsøe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars Ø. Pedersen, Hermogenes N. Jimenez, Søren M. Nielsen, Jesper M. Mathiesen, Hans Bräuner-Osborne Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-Bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-Selective Negative Allosteric Modulators Mol Pharmacol. 2012 Nov;82(5):929-37. doi: 10.1124/mol.112.078808. Epub 2012 Aug 16.
• DAVID C. RINKER, PATRICK L. JONES, R. JASON PITTS, MICHAEL RUTZLER, GRAY CAMP, LUJUAN SUN, PINGXI XU, DANIEL C. DORSET, DAVID WEAVER, LAURENCE J. ZWIEBEL Novel high-throughput screens of Anopheles gambiae odorant receptors reveal candidate behaviour-modifying chemicals for mosquitoes Physiol Entomol. 2012;37:33–41 doi: 10.1111/j.1365-3032.2011.00821.x
• Dinesh Puppala, Leon P. Collis, Sunny Z. Sun, Vinicius Bonato, Xian Chen, Blake Anson, Mathew Pletcher, Bernard Fermini, Sandra J. Engle Comparative Gene Expression Profiling in Human-Induced Pluripotent Stem Cell—Derived Cardiocytes and Human and Cynomolgus Heart Tissue Toxicol Sci. 2013 Jan;131(1):292-301. doi: 10.1093/toxsci/kfs282. Epub 2012 Sep 14.
• Franck Potet, Amanda N. Lorinc, Sebastien Chaigne, Corey R. Hopkins, Raghav Venkataraman, Svetlana Z. Stepanovic, L. Michelle Lewis, Emily Days, Veniamin Y. Sidorov, Darren W. Engers, Beiyan Zou, David Afshartous, Alfred L. George Jr., Courtney M. Campbell, Jeffrey R. Balser, Min Li, Franz J. Baudenbacher, Craig W. Lindsley, C. David Weaver, Sabina Kupershmidt Identification and Characterization of a Compound That Protects Cardiac Tissue from Human Ether-à-go-go-related Gene (hERG)-related Drug-induced Arrhythmias J Biol Chem. 2012 Nov 16;287(47):39613-25. doi: 10.1074/jbc.M112.380162. Epub 2012 Oct 2.
• Heinz Ruffner, Joëlle Sprunger, Olga Charlat, Juliet Leighton-Davies, Bianka Grosshans, Adrian Salathe, Svenja Zietzling, Valérie Beck, Maxime Therier, Andrea Isken, Yang Xie, Yue Zhang, Huaixiang Hao, Xiaoying Shi, Dong Liu, Qinhui Song, Ieuan Clay, Gabriele Hintzen, Jan Tchorz, Laure C. Bouchez, Gregory Michaud, Peter Finan, Vic E. Myer, Tewis Bouwmeester, Jeff Porter, Marc Hild, Fred Bassilana, Christian N. Parker, Feng Cong R-Spondin Potentiates Wnt/β-Catenin Signaling through Orphan Receptors LGR4 and LGR5 PLoS One. 2012;7(7):e40976. doi: 10.1371/journal.pone.0040976. Epub 2012 Jul 16.
• India C. Severin, Adriano L.S. Souza, Jonathan H. Davis, Najia Musolino, Matthias Mack, Christine A. Power, Amanda E.I. Proudfoot Properties of 7ND–CCL2 are modulated upon fusion to Fc Protein Eng Des Sel. 2012 May;25(5):213-22. doi: 10.1093/protein/gzs008. Epub 2012 Mar 2.
• Jack Bergman, Rebecca A. Roof, Cheryse A. Furman, Jennie L. Conroy, Nancy K. Mello, David R. Sibley, Phil Skolnick Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors Int J Neuropsychopharmacol. 2013 Mar;16(2):445-58. doi: 10.1017/S1461145712000661. Epub 2012 Jul 25.
• James M. Salovich, Paige N. Vinson, Douglas J. Sheffler, Atin Lamsal, Thomas J. Utley, Anna L. Blobaum, Thomas M. Bridges, Uyen Le, Carrie K. Jones, Michael R. Wood, J. Scott Daniels, P. Jeffrey Conn, Colleen M. Niswender, Craig W. Lindsley, Corey R. Hopkins Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor Bioorg Med Chem Lett. 2012 Aug 1;22(15):5084-8. doi: 10.1016/j.bmcl.2012.05.109. Epub 2012 Jun 6.
• Jingbo Xiao, R. Benjamin Free, Elena Barnaeva, Jennie Conroy, Trevor Doyle, Marthe Bryant-Genevier, Mercedes K. Taylor, Noel Southall, Xin Hu, Marc Ferrer, Steve Titus, Wei Zheng, David R. Sibley, Juan J. Marugan. Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 25 [updated 2013 Sep 03].
• Jung-eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Ki Hang Choi, Jahyo Kang, Eun Joo Roh Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers Bioorg Med Chem Lett. 2013 Mar 15;23(6):1887-90. doi: 10.1016/j.bmcl.2012.12.072. Epub 2013 Jan 12.
• Jutty Rajan Prashanth, Richard J. Lewis, Sébastien Dutertre Towards an integrated venomics approach for accelerated conopeptide discovery Toxicon. 2012 Sep 15;60(4):470-7. doi: 10.1016/j.toxicon.2012.04.340. Epub 2012 Apr 28.
• Linjie Chen, Lili Jin, Naiming Zhou An update of novel screening methods for GPCR in drug discovery Expert Opin Drug Discov. 2012 Sep;7(9):791-806. doi: 10.1517/17460441.2012.699036. Epub 2012 Jun 21.
• Mohammed Akhlaq; Elizabeth M. Rosethorne; Afrah Sattikar; Toby C. Kent The Use of Cold Plasma Technology to Reduce Carryover in Screening Assays J Lab Autom. 2013 Aug;18(4):269-75. doi: 10.1177/2211068212457780. Epub 2012 Sep 14.
• Nalin L. Subasinghe, Mark J. Wall, Michael P. Winters, Ning Qin, Mary Lou Lubin, Michael F.A. Finley, Michael R. Brandt, Michael P. Neeper, Craig R. Schneider, Raymond W. Colburn, Christopher M. Flores, Zhihua Sui A novel series of pyrazolylpiperidine N-type calcium channel blockers Bioorg Med Chem Lett. 2012 Jun 15;22(12):4080-3. doi: 10.1016/j.bmcl.2012.04.075. Epub 2012 May 2.
• Roman Hudec, Kozo Hamada, Katsuhiko Mikoshiba A fluorescence-based assay for the measurement of S-adenosylhomocysteine hydrolase activity in biological samples Anal Biochem. 2013 Feb 15;433(2):95-101. doi: 10.1016/j.ab.2012.10.014. Epub 2012 Oct 15.
• Shen Yin, Rocio Zamorano, P. Jeffrey Conn, Colleen M. Niswender Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors Neuropharmacology. 2013 Mar;66:122-32. doi: 10.1016/j.neuropharm.2012.03.003. Epub 2012 Mar 9.
• Wenthur C, Daniels JS, Morrison R, Engers JL, Niswender CM, Conn PJ, Lindsley CW. Development of a Second Generation mGlu3 NAM Probe Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 10 [updated 2013 Mar 22].
• Yueming Zheng, Xuejing Zhu, Pingzheng Zhou, Xi Lan, Haiyan Xu, Min Li, Zhaobing Gao Hexachlorophene Is a Potent KCNQ1/KCNE1 Potassium Channel Activator Which Rescues LQTs Mutants PLoS One. 2012;7(12):e51820. doi: 10.1371/journal.pone.0051820. Epub 2012 Dec 12.

2011

• Atsushi Inayoshi, Yoshiyuki Sugimoto, Jun Funahashi, Saori Takahashi, Masahiro Matsubara, Hideaki Kusaka Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker Life Sci. 2011 May 9;88(19-20):898-907. doi: 10.1016/j.lfs.2011.03.019. Epub 2011 Apr 3.
• C. David Weaver Triple-Addition Assay Protocols for Detecting and Characterizing Modulators of Seven-Transmembrane Receptors Curr Protoc Chem Biol. 2011 Sep 1;3(3):119-40. doi: 10.1002/9780470559277.ch110060.
• Carrie K. Jones, Michael Bubser, Analisa D. Thompson, Jonathan W. Dickerson, Nathalie Turle-Lorenzo, Marianne Amalric, Anna L. Blobaum, Thomas M. Bridges, Ryan D. Morrison, Satyawan Jadhav, Darren W. Engers, Kimberly Italiano, Jacob Bode, J. Scott Daniels, Craig W. Lindsley, Corey R. Hopkins, P. Jeffrey Conn, Colleen M. Niswender The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16.
• Curtis A. Thorne, Bonnie Lafleur, Michelle Lewis, Alison J. Hanson, Kristin K. Jernigan, David C. Weaver, Kari A. Huppert, Tony W. Chen, Chonlarat Wichadiit, Christopher S. Cselenyi, Emilios Tahinci, Kelly C. Meyers, Emily Waskow, Darren Orton, Adrian Salic, Laura A. Lee, David J. Robbins, Stacey S. Huppert, Ethan Lee A Biochemical Screen for Identification of Small-Molecule Regulators of the Wnt Pathway Using Xenopus Egg Extracts J Biomol Screen. 2011 Oct;16(9):995-1006. doi: 10.1177/1087057111416657. Epub 2011 Aug 21.
• Gaëlle Dintilhac, Deniz Arslan, Sébastien Dilly, Laurence Danober, Iuliana Botez, Pierre Lestage, Bernard Pirotte, Pascal de Tullio New substituted aryl esters and aryl amides of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors Med. Chem. Commun., 2011,2, 509-523 doi: 10.1039/C1MD00069A
• Haibo Yu, Meng Wu, Corey Hopkins, Julie Engers, Steve Townsend, Craig Lindsley, Owen B McManus, Min Li. A small molecule activator of KCNQ2 and KCNQ4 channels. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 29 [updated 2013 Feb 28].
• Haibo Yu, Kaiping Xu, Beiyan Zou, Meng Wu, Owen B. McManus, Julie Le Engers, Yiu-Yin Cheung, James M. Salovich, Corey R. Hopkins, Craig W. Lindsley, and Min Li. Identification of a novel, small molecule inhibitor of KCNQ2 channels Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Oct 28 [updated 2013 Feb 25].
• Haibo Yu, Zhihong Lin, Kaiping Xu, Xiaofang Huang, Shunyou Long, Meng Wu, Owen B. McManus, Julie Le Engers, Margrith E. Mattmann, Darren W. Engers, Uyen M. Le, Craig W. Lindsley, Corey R. Hopkins, Min Li. Identification of a novel, small molecule activator of KCNQ1 channels Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Dec 16 [updated 2013 Mar 7].
• Jacques Pantela, Savannah Y. Williams, Dehui Mi, Julien Sebag, Jackie D. Corbin, C. David Weaver, Roger D. Cone Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay Eur J Pharmacol. 2011 Jun 11;660(1):139-47. doi: 10.1016/j.ejphar.2011.01.031. Epub 2011 Feb 4.
• Jinghai Song, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Toshinori Ito Prevention of GVHD and graft rejection by a new S1P receptor agonist, W-061, in rat small bowel transplantation Transpl Immunol. 2012 Mar;26(2-3):163-70. doi: 10.1016/j.trim.2011.12.005. Epub 2011 Dec 14.
• Jun Chen, Regina M. Reilly, Philip R. Kym, and Shailen Joshi. In Vitro and in Vivo Assays for the Discovery of Analgesic Drugs Targeting TRP Channels In: Zhu MX, editor. TRP Channels. Boca Raton (FL): CRC Press; 2011. Chapter 18.
• Marianthi Papakosta, Carine Dalle, Alison Haythornthwaite, Lishuang Cao, Edward B. Stevens, Gillian Burgess, Rachel Russell, Peter J. Cox, Stephen C. Phillips, Christian Grimm The Chimeric Approach Reveals That Differences in the TRPV1 Pore Domain Determine Species-specific Sensitivity to Block of Heat Activation J Biol Chem. 2011 Nov 11;286(45):39663-72. doi: 10.1074/jbc.M111.273581. Epub 2011 Sep 12.
• Menghang Xia, Sampada A. Shahane, Ruili Huang, Steven A. Titus, Enoch Shum, Yong Zhao, Noel Southall, Wei Zheng, Kristine L. Witt, Raymond R. Tice, Christopher P. Austin Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels Toxicol Appl Pharmacol. 2011 May 1;252(3):250-8. doi: 10.1016/j.taap.2011.02.016. Epub 2011 Feb 26.
• Meredith J Noetzel, Jerri M Rook, Paige N Vinson, Hyekyung Cho, Emily Days, Y Zhou, Alice L Rodriguez, Hilde Lavreysen, Shaun R Stauffer, Colleen M Niswender, Zixiu Xiang, J Scott Daniels, Crag W Lindsley, C David Weaver, P Jeffrey Conn Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of mGlu5 in Regulating CNS Function Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21.
• Peter R McDonald, Anuradha Roy, Rathnam Chaguturu The University of Kansas High-Throughput Screening Laboratory. Part II: enabling collaborative drug-discovery partnerships through cutting-edge screening technology Future Med Chem. 2011 Jul;3(9):1101-10. doi: 10.4155/fmc.11.84.
• Rene Raphemot, Daniel F. Lonergan, Thuy T. Nguyen, Thomas Utley, L. Michelle Lewis, Rishin Kadakia, C. David Weaver, Rocco Gogliotti, Corey Hopkins, Craig W. Lindsley, Jerod S. Denton Discovery, characterization, and structure–activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X, and Kir7.1 Front Pharmacol. 2011 Nov 30;2:75. doi: 10.3389/fphar.2011.00075. eCollection 2011.
• Thierry Ferain, Hamid Hoveyda, Frédéric Ooms, Dominique Schols, Jérôme Bernard, Graeme Fraser Agonist-Induced Internalization of CC Chemokine Receptor 5 as a Mechanism to Inhibit HIV Replication J Pharmacol Exp Ther. 2011 Jun;337(3):655-62. doi: 10.1124/jpet.111.179622. Epub 2011 Mar 9.
• Xinmin Xie, John T. Brogan, Michael L. Schulte, Debbie Mi, Haibo Yu, Eric S. Dawson, Min Li, Owen McManus, Julie Engers, L. Michelle Lewis, Analisa Thompson, Carrie K. Jones, C. David Weaver, Craig W. Lindsley. Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 31 [updated 2013 Mar 22].
• Yasuaki Sanada, Tsunekazu Mizushima, Yasuyuki Kai, Junichi Nishimura, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Etsuko Uejima, Toshinori Ito Therapeutic Effects of Novel Sphingosine-1-Phosphate Receptor Agonist W-061 in Murine DSS Colitis PLoS One. 2011;6(9):e23933. doi: 10.1371/journal.pone.0023933. Epub 2011 Sep 8.

2010

• Ke Liu, Noel Southall, Steve A. Titus, James Inglese, Robert L. Eskay, Paul Shinn, Christopher P. Austin, Markus A. Heilig and Wei Zheng A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists. Assay Drug Dev Technol. 2010 Jun;8(3):367-79
• Brad P. Barnett, Yousang Hwang, Martin S. Taylor, Henriette Kirchner, Paul T. Pfluger, Vincent Bernard, Yu-yi Lin, Erin M. Bowers, Chandrani Mukherjee, Woo-Jin Song, Patti A. Longo, Daniel J. Leahy, Mehboob A. Hussain, Matthias H. Tschop, Jef D. Boeke and Philip A. Cole Glucose and Weight Control in Mice with a Designed Ghrelin O-Acyltransferase Inhibitor. Science 17 December 2010: Vol. 330 no. 6011 pp. 1689-1692
• Shuzo Watanabe, Masashi Ohmi, Tadashi Inoue, Chizu Nonomura, Akiyoshi Fujiuchi Identification of novel TRPM8 channel antagonists, Poster by RaQualia Pharma Inc.
• Evan P Lebois, Thomas M Bridges, L. Michelle Lewis, Eric S Dawson, Alexander S. Kane, Zixiu Xiang, Satyawan B Jadhav, Huiyong Yin, J. Phillip Kennedy, Jens Meiler, Colleen M. Niswender, Carrie K Jones, P Jeffrey Conn, C David Weaver, and Craig W Lindsley Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem Neurosci. 2010; 1(2): 104-121

2009

• Titus SA, Beacham D, Shahane SA, Southall N, Xia M, Huang R, Hooten E, Zhao Y, Shou L, Austin CP, Zheng W. A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel. Anal Biochem. 2009 Nov 1;394(1):30-8. Epub 2009 Jul 5
• Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.
• Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA. Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.
• Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorg Med Chem Lett. 2009 Feb 1;19(3):962-6. Epub 2008 Dec 25.
• Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype .Bioorg Med Chem Lett. 2009 Jun 15;19(12):3209-13. Epub 2009 May 3.
• Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Bioorg Med Chem Lett. 2009 Sep 1;19(17):4967-70. Epub 2009 Jul 18.
• Kim Y, Kang S, Lee JY, Rhim H. High throughput screening assay of alpha(1G) T-type Ca2+ channels and comparison with patch-clamp studies .Comb Chem High Throughput Screen. 2009 Mar;12(3):296-302.
• Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Curr Top Med Chem. 2009;9(13):1217-26.
• Mori T, Itami S, Yanagi T, Tatara Y, Takamiya M, Uchida T. Use of a Real-Time Fluorescence Monitoring System for High-Throughput Screening for Prolyl Isomerase Inhibitors. J Biomol Screen. 2009 Apr;14(4):419-24.
• Wise H, Abel PW, Cawkill D. Use of Reduced Temperature Cell Pausing to Enhance Flexibility of Cell-Based Assays. J Biomol Screen. 2009 Jul;14(6):716-22. Epub 2009 May 21.
• Sharma S, Kedrowski J, Rook JM, Smith RL, Jones CK, Rodriguez AL, Conn PJ, Lindsley CW. Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. J Med Chem. 2009 Jul 23;52(14):4103-6.
• Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
• Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8.
• Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. J Neurosci. 2009 Nov 11;29(45):14271-86.
• Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol Pharmacol. 2009 Aug;76(2):356-68. Epub 2009 Apr 30.
• Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol Pharmacol. 2009 Mar;75(3):577-88. Epub 2008 Dec 1.
• Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS. High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1. Mol Pharmacol. 2009 Nov;76(5):1094-103. Epub 2009 Aug 25.
• Irukayama-Tomobe Y, Tanaka H, Yokomizo T, Hashidate-Yoshida T, Yanagisawa M, Sakurai T. Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B. Proc Natl Acad Sci U S A. 2009 Mar 10;106(10):3930-4. Epub 2009 Feb 23.
• Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD.Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. Epub 2009 Mar 11.

2008

• Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg Med Chem Lett. 2008 Feb 1;18(3):885-90. Epub 2008 Jan 4.
• Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. Epub 2008 Aug 29.
• Kim HJ, Yun HM, Kim T, Nam G, Roh EJ, Kostenis E, Choo HY, Pae AN, Rhim H. Functional human 5-HT6 receptor assay for high throughput screening of chemical ligands and binding proteins. Comb Chem High Throughput Screen. 2008 May;11(4):316-24.
• Gunnet JW, Wines P, Xiang M, Rybczynski P, Andrade-Gordon P, de Garavilla L, Parry TJ, Cheung WM, Minor L, Demarest KT, Maryanoff BE, Damiano BP. Pharmacological characterization of RWJ-676070, a dual vasopressin V(1A)/V(2) receptor antagonist. Eur J Pharmacol. 2008 Aug 20;590(1-3):333-42. Epub 2008 Jun 7.
• Akasofu S, Sawada K, Kosasa T, Hihara H, Ogura H, Akaike A. Donepezil attenuates excitotoxic damage induced by membrane depolarization of cortical neurons exposed to veratridine. Eur J Pharmacol. 2008 Jul 7;588(2-3):189-97. Epub 2008 Apr 13.
• Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33.
• Kobayashi K, Nishizawa Y, Sawada K, Ogura H, Miyabe M. K(+)-channel openers suppress epileptiform activities induced by 4-aminopyridine in cultured rat hippocampal neurons. Pharmacol Sci. 2008 Dec;108(4):517-28. Epub 2008 Dec 11.
• Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Pharmacol. 2008 Apr;73(4):1213-24. Epub 2008 Jan 2.
• Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58. Epub 2008 Jul 29.
• Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol. 2008 Jan;4(1):42-50. Epub 2007 Dec 2.
• Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ. Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated Neuropharmacology. 2008 Apr;54(5):804-14. Epub 2007 Dec 24.
• Taniguchi Y, Tonai-Kachi H, Shinjo K. 5-Nitro-2-(3-phenylpropylamino)benzoic acid is a GPR35 agonist Pharmacology. 2008;82(4):245-9. Epub 2008 Sep 26.

2007

• Park JH, Choi JK, Lee E, Lee JK, Rhim H, Seo SH, Kim Y, Doddareddy MR, Pae AN, Kang J, Roh EJ. Lead discovery and optimization of T-type calcium channel blockers Bioorg Med Chem. 2007 Feb 1;15(3):1409-19. Epub 2006 Nov 10.
• Yun HM, Kim S, Kim HJ, Kostenis E, Kim JI, Seong JY, Baik JH, Rhim H. The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn . J Biol Chem. 2007 Feb 23;282(8):5496-505. Epub 2006 Dec 22.
• Cassutt KJ, Orsini MJ, Abousleiman M, Colone D, Tang W. Identifying Nonselective Hits from a Homogeneous Calcium Assay Screen J Biomol Screen. 2007 Mar;12(2):285-7. Epub 2007 Feb 8.
• Song F, Lu S, Gunnet J, Xu JZ, Wines P, Proost J, Liang Y, Baumann C, Lenhard J, Murray WV, Demarest KT, Kuo GH. Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists J Med Chem. 2007 Jun 14;50(12):2807-17. Epub 2007 May 15.
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2006

• Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A
• Protective effect of donepezil in primary-cultured rat cortical neurons exposed to N-methyl-d-aspartate (NMDA) toxicity
• Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35
• A neuropeptide ligand of the G protein-coupled receptor GPR103 regulates feeding, behavioral arousal, and blood pressure in mice

2005

• SOX6 attenuates glucose-stimulated insulin secretion by repressing PDX1 transcriptional activity and is down-regulated in hyperinsulinemic obese mice
• Tissue transglutaminase-mediated formation and cleavage of histamine-gliadin complexes: biological effects and implications for celiac disease
• A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
• Functional role of prostacyclin receptor in rat dorsal root ganglion neurons

2004

• Stimulation of increases in intracellular calcium and prostaglandin E2 generation in Chinese hamster ovary cells expressing receptor-Galpha16 fusion proteins
• Identification and characterization of a cell-surface receptor, P2Y15, for AMP and adenosine

2003

• Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation

2002

• Identification of a potent and orally active non-peptide C5a receptor antagonist
• Adaptation of Aequorin Functional Assay to High Throughput Screening

2001

• Potent and selective inhibition of the human Na+/H+ exchanger isoform NHE1 by a novel aminoguanidine derivative T-162559
• Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5