Profile

My research is focused on the discovery and characterization of novel chemical tools for studying ion channel structure, function, and therapeutic potential. Specifically, the projects in my lab are focused on two key roles of ion channels in medicine and public health. The first project area deals with development of drug-like chemical tools for evaluating the role of ligand and voltage-activated potassium channels for the treatment of pain, one the largest unmet medical needs. Recent discoveries in the laboratory are paving the way for the field's first opportunites to evaluate a novel ion channel pain target. The second project area deals with the development of novel insecticides to aid in the control of malaria and other mosquito-born illnesses that infect nearly half a billion and kill over 1 million people every year. Another recent advancement in high-throughput ion channel assay technology from the laboratory is now making it possibly to rapidly discover and develop novel insecticide to combat the resistance that has developed in insects to the insecticides that were so effective in helping erradicate malaria from the United States and Australia in the middle of the 20th century. The techniques most most commonly used in the laboratory are plate-based fluorescent assays of ion channel function, automated high-throughput screening, and whole-cell electrophysiology. My laboratory collaborates closely with medicinal chemists, imformaticians, structural biologists, engineers, and software developers.

Publications

The following timeline graph is generated from all co-authored publications.

Featured publications are shown below:

  1. Functional Coupling of K-Cl Cotransporter (KCC) to GABA-Gated Cl Channels in the Central Nervous System of Drosophila melanogaster Leads to Altered Drug Sensitivities. Chen R, Prael FJ, Li Z, Delpire E, Weaver CD, Swale DR (2019) ACS Chem Neurosci 10(6): 2765-2776
    › Primary publication · 30942574 (PubMed)
  2. VU0810464, a non-urea G protein-gated inwardly rectifying K (K 3/GIRK) channel activator, exhibits enhanced selectivity for neuronal K 3 channels and reduces stress-induced hyperthermia in mice. Vo BN, Abney KK, Anderson A, Marron Fernandez de Velasco E, Benneyworth MA, Daniels JS, Morrison RD, Hopkins CR, Weaver CD, Wickman K (2019) Br J Pharmacol 176(13): 2238-2249
    › Primary publication · 30924523 (PubMed) · PMC6555862 (PubMed Central)
  3. Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models. Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD (2019) ACS Chem Neurosci 10(5): 2621
    › Primary publication · 30912639 (PubMed)
  4. Use of chemical probes to explore the toxicological potential of the K/Cl cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti. Prael FJ, Chen R, Li Z, Reed CW, Lindsley CW, Weaver CD, Swale DR (2018) Pestic Biochem Physiol : 10-17
    › Primary publication · 30704707 (PubMed)
  5. Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models. Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Linsdley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD (2019) ACS Chem Neurosci 10(3): 1294-1299
    › Primary publication · 30474955 (PubMed)
  6. Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-Gated, Inwardly Rectifying, Potassium (GIRK) Channels. Kozek KA, Du Y, Sharma S, Prael FJ, Spitznagel BD, Kharade SV, Denton JS, Hopkins CR, Weaver CD (2019) ACS Chem Neurosci 10(1): 358-370
    › Primary publication · 30136838 (PubMed) · PMC6528656 (PubMed Central)
  7. Rhodol-based thallium sensors for cellular imaging of potassium channel activity. Dutter BF, Ender A, Sulikowski GA, Weaver CD (2018) Org Biomol Chem 16(31): 5575-5579
    › Primary publication · 30051127 (PubMed) · PMC6151185 (PubMed Central)
  8. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS (2018) Mol Pharmacol 94(2): 926-937
    › Primary publication · 29895592 (PubMed) · PMC6041953 (PubMed Central)
  9. Selective Activation of N,N'-Diacyl Rhodamine Pro-fluorophores Paired with Releasing Enzyme, Porcine Liver Esterase (PLE). Abney KK, Ramos-Hunter SJ, Romaine IM, Goodwin JS, Sulikowski GA, Weaver CD (2018) Chemistry 24(36): 8985-8988
    › Primary publication · 29679472 (PubMed) · PMC6035858 (PubMed Central)
  10. Identification and Characterization of the First Selective Y Receptor Positive Allosteric Modulator. Schubert M, Stichel J, Du Y, Tough IR, Sliwoski G, Meiler J, Cox HM, Weaver CD, Beck-Sickinger AG (2017) J Med Chem 60(17): 7605-7612
    › Primary publication · 28795803 (PubMed)
  11. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators. Wieting JM, Vadukoot AK, Sharma S, Abney KK, Bridges TM, Daniels JS, Morrison RD, Wickman K, Weaver CD, Hopkins CR (2017) ACS Chem Neurosci 8(9): 1873-1879
    › Primary publication · 28697302 (PubMed) · PMC6116837 (PubMed Central)
  12. Optical control of neuronal activity using a light-operated GIRK channel opener (LOGO). Barber DM, Schönberger M, Burgstaller J, Levitz J, Weaver CD, Isacoff EY, Baier H, Trauner D (2016) Chem Sci 7(3): 2347-2352
    › Primary publication · 28090283 (PubMed) · PMC5234268 (PubMed Central)
  13. Optical control of GIRK channels using visible light. Trads JB, Burgstaller J, Laprell L, Konrad DB, de la Osa de la Rosa L, Weaver CD, Baier H, Trauner D, Barber DM (2016) Org Biomol Chem 15(1): 76-81
    › Primary publication · 27901161 (PubMed)
  14. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW (2014) J Med Chem 57(23): 10192-7
    › Primary publication · 25423411 (PubMed) · PMC4266362 (PubMed Central)
  15. Discovery of potent and selective GIRK1/2 modulators via 'molecular switches' within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas. Wen W, Wu W, Weaver CD, Lindsley CW (2014) Bioorg Med Chem Lett 24(21): 5102-6
    › Primary publication · 25264075 (PubMed)
  16. Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7. Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, Walker AG, Melancon BJ, Wood MR, Lindsley CW, Conn PJ, Xiang Z, Hopkins CR, Niswender CM (2014) ACS Chem Neurosci 5(12): 1221-37
    › Primary publication · 25225882 (PubMed) · PMC4306484 (PubMed Central)
  17. Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297. Wydeven N, Marron Fernandez de Velasco E, Du Y, Benneyworth MA, Hearing MC, Fischer RA, Thomas MJ, Weaver CD, Wickman K (2014) Proc Natl Acad Sci U S A 111(29): 10755-60
    › Primary publication · 25002517 (PubMed) · PMC4115558 (PubMed Central)
  18. Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅). Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR (2014) J Med Chem 57(13): 5620-37
    › Primary publication · 24914612 (PubMed) · PMC4096224 (PubMed Central)
  19. A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors. Morris LC, Days EL, Turney M, Mi D, Lindsley CW, Weaver CD, Niswender KD (2014) J Biomol Screen 19(6): 847-58
    › Primary publication · 24525870 (PubMed) · PMC4306651 (PubMed Central)
  20. N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK (2013) J Pharmacol Exp Ther 347(2): 438-57
    › Primary publication · 23965381 (PubMed) · PMC3807069 (PubMed Central)
  21. Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor. Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T (2013) J Med Chem 56(18): 7243-59
    › Primary publication · 23947773 (PubMed) · PMC3924858 (PubMed Central)
  22. Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA (2013) Bioorg Med Chem Lett 23(18): 5195-8
    › Primary publication · 23916258 (PubMed) · PMC4066871 (PubMed Central)
  23. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Wen W, Wu W, Romaine IM, Kaufmann K, Du Y, Sulikowski GA, Weaver CD, Lindsley CW (2013) Bioorg Med Chem Lett 23(16): 4562-6
    › Primary publication · 23838260 (PubMed) · PMC3816575 (PubMed Central)
  24. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, Lindsley CW, Weaver CD (2013) ACS Chem Neurosci 4(9): 1278-86
    › Primary publication · 23730969 (PubMed) · PMC3778424 (PubMed Central)
  25. Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. Zhou Y, Manka JT, Rodriguez AL, Weaver CD, Days EL, Vinson PN, Jadhav S, Hermann EJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR (2010) ACS Med Chem Lett 1(8): 433-438
    › Primary publication · 23308336 (PubMed) · PMC3539763 (PubMed Central)
  26. Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR (2012) Bioorg Med Chem Lett 22(24): 7388-92
    › Primary publication · 23142615 (PubMed) · PMC3539767 (PubMed Central)
  27. Nonoisotopic assay for the presynaptic choline transporter reveals capacity for allosteric modulation of choline uptake. Ruggiero AM, Wright J, Ferguson SM, Lewis M, Emerson KS, Iwamoto H, Ivy MT, Holmstrand EC, Ennis EA, Weaver CD, Blakely RD (2012) ACS Chem Neurosci 3(10): 767-81
    › Primary publication · 23077721 (PubMed) · PMC3474274 (PubMed Central)
  28. Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias. Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL, Campbell CM, Balser JR, Li M, Baudenbacher FJ, Lindsley CW, Weaver CD, Kupershmidt S (2012) J Biol Chem 287(47): 39613-25
    › Primary publication · 23033485 (PubMed) · PMC3501040 (PubMed Central)
  29. Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR (2012) Bioorg Med Chem Lett 22(20): 6481-5
    › Primary publication · 22981332 (PubMed) · PMC3755010 (PubMed Central)
  30. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Delpire E, Baranczak A, Waterson AG, Kim K, Kett N, Morrison RD, Daniels JS, Weaver CD, Lindsley CW (2012) Bioorg Med Chem Lett 22(14): 4532-5
    › Primary publication · 22727639 (PubMed) · PMC3389279 (PubMed Central)
  31. A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer. Blättermann S, Peters L, Ottersbach PA, Bock A, Konya V, Weaver CD, Gonzalez A, Schröder R, Tyagi R, Luschnig P, Gäb J, Hennen S, Ulven T, Pardo L, Mohr K, Gütschow M, Heinemann A, Kostenis E (2012) Nat Chem Biol 8(7): 631-8
    › Primary publication · 22634634 (PubMed)
  32. Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators. Mueller R, Dawson ES, Niswender CM, Butkiewicz M, Hopkins CR, Weaver CD, Lindsley CW, Conn PJ, Meiler J (2012) J Mol Model 18(9): 4437-46
    › Primary publication · 22592386 (PubMed) · PMC3766737 (PubMed Central)
  33. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, Dawson ES, Li M, McManus O, Jones CK, Daniels JS, Hopkins CR, Xie XS, Conn PJ, Weaver CD, Lindsley CW (2011) ACS Chem Neurosci 2(12): 730-742
    › Primary publication · 22368764 (PubMed) · PMC3285241 (PubMed Central)
  34. 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. Raphemot R, Lonergan DF, Nguyen TT, Utley T, Lewis LM, Kadakia R, Weaver CD, Gogliotti R, Hopkins C, Lindsley CW, Denton JS (2011) Front Pharmacol : 75
    › Primary publication · 22275899 (PubMed) · PMC3254186 (PubMed Central)
  35. MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines. Aldrich LN, Lebois EP, Lewis LM, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW (2009) Tetrahedron Lett 50(2): 212-215
    › Primary publication · 22090663 (PubMed) · PMC3214729 (PubMed Central)
  36. Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, Conn PJ (2012) Mol Pharmacol 81(2): 120-33
    › Primary publication · 22021324 (PubMed) · PMC3263948 (PubMed Central)
  37. Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model. Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR (2011) J Med Chem 54(21): 7639-47
    › Primary publication · 21966889 (PubMed) · PMC3226828 (PubMed Central)
  38. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. Lebois EP, Bridges TM, Lewis LM, Dawson ES, Kane AS, Xiang Z, Jadhav SB, Yin H, Kennedy JP, Meiler J, Niswender CM, Jones CK, Conn PJ, Weaver CD, Lindsley CW (2010) ACS Chem Neurosci 1(2): 104-121
    › Primary publication · 21961051 (PubMed) · PMC3180826 (PubMed Central)
  39. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. Miller M, Shi J, Zhu Y, Kustov M, Tian JB, Stevens A, Wu M, Xu J, Long S, Yang P, Zholos AV, Salovich JM, Weaver CD, Hopkins CR, Lindsley CW, McManus O, Li M, Zhu MX (2011) J Biol Chem 286(38): 33436-46
    › Primary publication · 21795696 (PubMed) · PMC3190871 (PubMed Central)
  40. High-throughput quantification of bioactive lipids by MALDI mass spectrometry: application to prostaglandins. Manna JD, Reyzer ML, Latham JC, Weaver CD, Marnett LJ, Caprioli RM (2011) Anal Chem 83(17): 6683-8
    › Primary publication · 21770391 (PubMed) · PMC3165080 (PubMed Central)
  41. Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄. Cheung YY, Zamorano R, Blobaum AL, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR (2011) ACS Comb Sci 13(2): 159-65
    › Primary publication · 21338051 (PubMed) · PMC3057427 (PubMed Central)
  42. Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Williams R, Manka JT, Rodriguez AL, Vinson PN, Niswender CM, Weaver CD, Jones CK, Conn PJ, Lindsley CW, Stauffer SR (2011) Bioorg Med Chem Lett 21(5): 1350-3
    › Primary publication · 21315585 (PubMed) · PMC3498823 (PubMed Central)
  43. Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay. Pantel J, Williams SY, Mi D, Sebag J, Corbin JD, Weaver CD, Cone RD (2011) Eur J Pharmacol 660(1): 139-47
    › Primary publication · 21296065 (PubMed) · PMC3175485 (PubMed Central)
  44. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR (2011) J Med Chem 54(4): 1106-10
    › Primary publication · 21247167 (PubMed) · PMC3166797 (PubMed Central)
  45. Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW (2011) ACS Chem Biol 6(5): 452-65
    › Primary publication · 21241068 (PubMed) · PMC3401128 (PubMed Central)
  46. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR (2011) Bioorg Med Chem Lett 21(9): 2697-701
    › Primary publication · 21194936 (PubMed) · PMC3082000 (PubMed Central)
  47. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Bhave G, Chauder BA, Liu W, Dawson ES, Kadakia R, Nguyen TT, Lewis LM, Meiler J, Weaver CD, Satlin LM, Lindsley CW, Denton JS (2011) Mol Pharmacol 79(1): 42-50
    › Primary publication · 20926757 (PubMed) · PMC3014278 (PubMed Central)
  48. Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Rodriguez AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ (2010) Mol Pharmacol 78(6): 1105-23
    › Primary publication · 20923853 (PubMed) · PMC2993468 (PubMed Central)
  49. Identification of Small Molecule Inhibitors of Clostridium perfringens ε-Toxin Cytotoxicity Using a Cell-Based High-Throughput Screen. Lewis M, Weaver CD, McClain MS (2010) Toxins (Basel) 2(7): 1825-1847
    › Primary publication · 20721308 (PubMed) · PMC2922765 (PubMed Central)
  50. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR (2010) Bioorg Med Chem Lett 20(17): 5175-8
    › Primary publication · 20667732 (PubMed) · PMC2922490 (PubMed Central)
  51. Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening. Mueller R, Rodriguez AL, Dawson ES, Butkiewicz M, Nguyen TT, Oleszkiewicz S, Bleckmann A, Weaver CD, Lindsley CW, Conn PJ, Meiler J (2010) ACS Chem Neurosci 1(4): 288-305
    › Primary publication · 20414370 (PubMed) · PMC2857954 (PubMed Central)
  52. Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7. Niswender CM, Johnson KA, Miller NR, Ayala JE, Luo Q, Williams R, Saleh S, Orton D, Weaver CD, Conn PJ (2010) Mol Pharmacol 77(3): 459-68
    › Primary publication · 20026717 (PubMed) · PMC2835423 (PubMed Central)
  53. Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW (2009) Bioorg Med Chem Lett 19(23): 6502-6
    › Primary publication · 19875287 (PubMed) · PMC3177597 (PubMed Central)
  54. Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA (2009) Bioorg Med Chem Lett 19(23): 6623-6
    › Primary publication · 19854049 (PubMed) · PMC2801349 (PubMed Central)
  55. 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. 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 (2009) Curr Top Med Chem 9(13): 1217-26
    › Primary publication · 19807667 (PubMed) · PMC4765323 (PubMed Central)
  56. High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1. Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS (2009) Mol Pharmacol 76(5): 1094-103
    › Primary publication · 19706730 (PubMed) · PMC2774996 (PubMed Central)
  57. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR (2009) Bioorg Med Chem Lett 19(17): 4967-70
    › Primary publication · 19640716 (PubMed) · PMC2752865 (PubMed Central)
  58. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR (2009) J Med Chem 52(14): 4115-8
    › Primary publication · 19469556 (PubMed) · PMC2765192 (PubMed Central)
  59. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW (2009) Bioorg Med Chem Lett 19(12): 3209-13
    › Primary publication · 19443219 (PubMed) · PMC3177605 (PubMed Central)
  60. 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. Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW (2009) J Med Chem 52(11): 3445-8
    › Primary publication · 19438238 (PubMed) · PMC3875304 (PubMed Central)
  61. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. 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 (2009) Mol Pharmacol 76(2): 356-68
    › Primary publication · 19407080 (PubMed) · PMC2713127 (PubMed Central)
  62. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD (2009) Proc Natl Acad Sci U S A 106(13): 5383-8
    › Primary publication · 19279215 (PubMed) · PMC2654392 (PubMed Central)
  63. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. 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 (2009) Mol Pharmacol 75(3): 577-88
    › Primary publication · 19047481 (PubMed) · PMC2684909 (PubMed Central)
  64. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. 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 (2008) Mol Pharmacol 74(5): 1345-58
    › Primary publication · 18664603 (PubMed) · PMC2574552 (PubMed Central)
  65. Application of combinatorial chemistry science on modern drug discovery. Kennedy JP, Williams L, Bridges TM, Daniels RN, Weaver D, Lindsley CW (2008) J Comb Chem 10(3): 345-54
    › Primary publication · 18220367 (PubMed)
  66. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. 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 (2008) Bioorg Med Chem Lett 18(3): 885-90
    › Primary publication · 18178088 (PubMed) · PMC2275053 (PubMed Central)
  67. 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. Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD (2008) Mol Pharmacol 73(4): 1213-24
    › Primary publication · 18171729 (PubMed)
  68. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ (2008) Nat Chem Biol 4(1): 42-50
    › Primary publication · 18059262 (PubMed)
  69. Preclinical drug discovery research and training at Vanderbilt. Lindsley CW, Weaver D, Jones C, Marnett L, Conn PJ (2007) ACS Chem Biol 2(1): 17-20
    › Primary publication · 17243778 (PubMed)