| Year |
Citation |
Score |
| 2023 |
Qi A, Kling HE, Billard N, Rodriguez AL, Peng L, Dickerson JW, Engers JL, Bender AM, Moehle MS, Lindsley CW, Rook JM, Niswender CM. . Molecular Pharmacology. PMID 37595966 DOI: 10.1124/molpharm.122.000643 |
0.36 |
|
| 2023 |
Lei X, Hofmann C, Rodriguez AL, Niswender C. Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7. Molecular Pharmacology. PMID 37105671 DOI: 10.1124/molpharm.123.000678 |
0.385 |
|
| 2022 |
Kalbfleisch JJ, Rodriguez AL, Lei X, Weiss K, Blobaum AL, Boutaud O, Niswender CM, Lindsley CW. Persistent challenges in the development of an mGlu PAM in vivo tool compound: The discovery of VU6046980. Bioorganic & Medicinal Chemistry Letters. 80: 129106. PMID 36528230 DOI: 10.1016/j.bmcl.2022.129106 |
0.368 |
|
| 2022 |
Orsi DL, Felts AS, Rodriguez AL, Vinson PN, Cho HP, Chang S, Blobaum AL, Niswender CM, Jeffrey Conn P, Jones CK, Lindsley CW, Han C. Discovery of a potent M antagonist with improved clearance profile. Part 2: pyrrolidine amide-based antagonists. Bioorganic & Medicinal Chemistry Letters. 129021. PMID 36228968 DOI: 10.1016/j.bmcl.2022.129021 |
0.346 |
|
| 2022 |
Capstick RA, Whomble D, Orsi DL, Felts AS, Rodriguez AL, Vinson PN, Chang S, Blobaum AL, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Discovery of a potent M antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorganic & Medicinal Chemistry Letters. 76: 128988. PMID 36113671 DOI: 10.1016/j.bmcl.2022.128988 |
0.346 |
|
| 2022 |
Reed CW, Rodriguez AL, Kalbfleisch JJ, Seto M, Jenkins MT, Blobaum AL, Chang S, Lindsley CW, Niswender CM. Development and profiling of mGlu NAMs with a range of saturable inhibition of agonist responses in vitro. Bioorganic & Medicinal Chemistry Letters. 74: 128923. PMID 35944850 DOI: 10.1016/j.bmcl.2022.128923 |
0.422 |
|
| 2021 |
Barbaro L, Rodriguez AL, Blevins AN, Dickerson JW, Billard N, Boutaud O, Rook JL, Niswender CM, Conn PJ, Engers DW, Lindsley CW. Discovery of "Molecular Switches" within a Series of mGlu Allosteric Ligands Driven by a "Magic Methyl" Effect Affording Both PAMs and NAMs with Activity, Derived from an M PAM Chemotype. Acs Bio & Med Chem Au. 1: 21-30. PMID 37101980 DOI: 10.1021/acsbiomedchemau.1c00024 |
0.363 |
|
| 2021 |
Bender AM, Carter TR, Spock M, Rodriguez AL, Dickerson JW, Rook JM, Chang S, Qi A, Presley CC, Engers DW, Harp JM, Bridges TM, Niswender CM, Conn PJ, Lindsley CW. Synthesis and Characterization of Chiral 6-Azaspiro[2.5]Octanes as Potent and Selective Antagonists of the M Muscarinic Acetylcholine Receptor. Bioorganic & Medicinal Chemistry Letters. 128479. PMID 34838649 DOI: 10.1016/j.bmcl.2021.128479 |
0.369 |
|
| 2021 |
Yamada Y, Gilliland K, Xiang Z, Haymer D, Crocker KE, Loch MT, Schulte ML, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Melancon BJ. Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds. Bioorganic & Medicinal Chemistry Letters. 128342. PMID 34461178 DOI: 10.1016/j.bmcl.2021.128342 |
0.37 |
|
| 2021 |
Moehle MS, Bender AM, Dickerson JW, Foster DJ, Qi A, Cho HP, Donsante Y, Peng W, Bryant Z, Stillwell KJ, Bridges TM, Chang S, Watson KJ, O'Neill JC, Engers JL, ... ... Rodriguez AL, et al. Discovery of the First Selective M Muscarinic Acetylcholine Receptor Antagonists with Antiparkinsonian and Antidystonic Efficacy. Acs Pharmacology & Translational Science. 4: 1306-1321. PMID 34423268 DOI: 10.1021/acsptsci.0c00162 |
0.328 |
|
| 2021 |
Spock M, Carter TR, Bollinger KA, Han C, Baker LA, Rodriguez AL, Peng L, Dickerson JW, Qi A, Rook JM, O'Neill JC, Watson KJ, Chang S, Bridges TM, Engers JL, et al. Discovery of VU6028418: A Highly Selective and Orally Bioavailable M Muscarinic Acetylcholine Receptor Antagonist. Acs Medicinal Chemistry Letters. 12: 1342-1349. PMID 34413964 DOI: 10.1021/acsmedchemlett.1c00363 |
0.348 |
|
| 2021 |
Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Discovery of a Novel Class of Heteroaryl-Pyrrolidinones as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M. Bioorganic & Medicinal Chemistry Letters. 128193. PMID 34118412 DOI: 10.1016/j.bmcl.2021.128193 |
0.302 |
|
| 2020 |
Davis DC, Bungard JD, Chang S, Rodriguez AL, Blobaum AL, Boutaud O, Melancon BJ, Niswender CM, Jeffrey Conn P, Lindsley CW. Lead optimization of the VU0486321 series of mGlu PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs. Bioorganic & Medicinal Chemistry Letters. 127724. PMID 33253881 DOI: 10.1016/j.bmcl.2020.127724 |
0.459 |
|
| 2020 |
Reed CW, Kalbfleisch JJ, Wong MJ, Washecheck JP, Hunter A, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu Positive Allosteric Modulator Tool Compound. Acs Medicinal Chemistry Letters. 11: 1773-1779. PMID 32944146 DOI: 10.1021/Acsmedchemlett.0C00432 |
0.371 |
|
| 2020 |
Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW. Synthesis and SAR of a series of mGlu NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core. Bioorganic & Medicinal Chemistry Letters. 127529. PMID 32890686 DOI: 10.1016/J.Bmcl.2020.127529 |
0.431 |
|
| 2020 |
Fulton MG, Loch MT, Rodriguez AL, Lin X, Javitch JA, Conn PJ, Niswender CM, Lindsley CW. Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu heterodimeric receptor results in a compound with mGlu homodimer selectivity. Bioorganic & Medicinal Chemistry Letters. 127212. PMID 32371100 DOI: 10.1016/J.Bmcl.2020.127212 |
0.534 |
|
| 2019 |
Fulton MG, Loch MT, Cuoco CA, Rodriguez AL, Days E, Vinson PN, Kozek KA, Weaver CD, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Challenges in the Discovery and Optimization of mGlu Heterodimer Positive Allosteric Modulators. Letters in Drug Design & Discovery. 16: 1387-1394. PMID 32201485 DOI: 10.2174/1570180815666181017131349 |
0.312 |
|
| 2019 |
Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes. Bioorganic & Medicinal Chemistry Letters. 126811. PMID 31787491 DOI: 10.1016/J.Bmcl.2019.126811 |
0.306 |
|
| 2019 |
Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotype. Bioorganic & Medicinal Chemistry Letters. 126812. PMID 31784320 DOI: 10.1016/J.Bmcl.2019.126812 |
0.342 |
|
| 2019 |
Yamada Y, Yohn SE, Gilliland K, Loch MT, Schulte ML, Rodriguez AL, Blobaum AL, Niswender CM, Jeffrey Conn P, Lindsley CW. Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy. Bioorganic & Medicinal Chemistry Letters. PMID 31358468 DOI: 10.1016/J.Bmcl.2019.07.030 |
0.385 |
|
| 2019 |
Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, et al. SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M PAMs. Bioorganic & Medicinal Chemistry Letters. PMID 31248774 DOI: 10.1016/J.Bmcl.2019.06.032 |
0.355 |
|
| 2019 |
Butkiewicz M, Rodriguez AL, Rainey SE, Wieting JM, Luscombe VB, Stauffer SR, Lindsley CW, Conn PJ, Meiler J. Identification of novel allosteric modulators of mGlu5 acting at site distinct from MPEP binding. Acs Chemical Neuroscience. PMID 31132237 DOI: 10.1021/Acschemneuro.8B00227 |
0.5 |
|
| 2019 |
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, et al. VU6005806/AZN-00016130, an advanced M positive allosteric modulator (PAM) profiled as a potential preclinical development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 31113706 DOI: 10.1016/J.Bmcl.2019.05.026 |
0.354 |
|
| 2019 |
Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW. Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278. Bioorganic & Medicinal Chemistry Letters. PMID 30910459 DOI: 10.1016/J.Bmcl.2019.03.016 |
0.363 |
|
| 2019 |
Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, et al. Discovery of VU2957 (Valiglurax): An mGlu Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. Acs Medicinal Chemistry Letters. 10: 255-260. PMID 30891122 DOI: 10.1021/Acsmedchemlett.8B00426 |
0.332 |
|
| 2019 |
Reed CW, Yohn S, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 Negative Allosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). Journal of Medicinal Chemistry. PMID 30608678 DOI: 10.1021/Acs.Jmedchem.8B01810 |
0.392 |
|
| 2018 |
Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Jeffrey Conn P, Lindsley CW. Novel M positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands. Bioorganic & Medicinal Chemistry Letters. PMID 30580918 DOI: 10.1016/J.Bmcl.2018.12.039 |
0.316 |
|
| 2018 |
Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, ... Rodriguez AL, et al. The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 30503632 DOI: 10.1016/J.Bmcl.2018.10.050 |
0.377 |
|
| 2018 |
Felts AS, Bollinger KA, Brassard CJ, Rodriguez AL, Morrison RD, Scott Daniels J, Blobaum AL, Niswender CM, Jones CK, Jeffrey Conn P, Emmitte KA, Lindsley CW. Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 30446311 DOI: 10.1016/J.Bmcl.2018.11.017 |
0.421 |
|
| 2018 |
Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW. Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) based on functionalized pyrazolo[1,5- a]pyrimidine-5-carboxamide and thieno[3,2- b]pyridine-5-carboxamide cores. Journal of Medicinal Chemistry. PMID 30350962 DOI: 10.1021/Acs.Jmedchem.8B01266 |
0.483 |
|
| 2018 |
Bollinger S, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. The discovery, SAR and biological characterization of a novel series of 6-((1H-pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Journal of Medicinal Chemistry. PMID 30247901 DOI: 10.1021/Acs.Jmedchem.8B00994 |
0.401 |
|
| 2018 |
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, et al. Corrigendum to "Challenges in the development of an M PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]. Bioorganic & Medicinal Chemistry Letters. PMID 30076050 DOI: 10.1016/J.Bmcl.2018.07.022 |
0.348 |
|
| 2018 |
Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, et al. Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu positive allosteric modulators that mitigate CYP1A2 induction liability. Bioorganic & Medicinal Chemistry Letters. PMID 29958762 DOI: 10.1016/J.Bmcl.2018.06.034 |
0.409 |
|
| 2018 |
Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 29705142 DOI: 10.1016/J.Bmcl.2018.04.053 |
0.489 |
|
| 2017 |
Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, et al. VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides. Acs Medicinal Chemistry Letters. 8: 1326-1330. PMID 29259756 DOI: 10.1021/Acsmedchemlett.7B00429 |
0.338 |
|
| 2017 |
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, et al. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides. Bioorganic & Medicinal Chemistry Letters. PMID 29089231 DOI: 10.1016/J.Bmcl.2017.10.053 |
0.405 |
|
| 2017 |
Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. Acs Medicinal Chemistry Letters. 8: 1110-1115. PMID 29057060 DOI: 10.1021/Acsmedchemlett.7B00317 |
0.492 |
|
| 2017 |
Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping. Bioorganic & Medicinal Chemistry Letters. PMID 29037946 DOI: 10.1016/J.Bmcl.2017.10.016 |
0.355 |
|
| 2017 |
Felts AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 28958625 DOI: 10.1016/J.Bmcl.2017.09.042 |
0.478 |
|
| 2017 |
Engers JL, Bollinger KA, Weiner RL, Rodriguez AL, Long MF, Breiner MM, Chang S, Bollinger SR, Bubser M, Jones CK, Morrison RD, Bridges TM, Blobaum AL, Niswender CM, Conn PJ, et al. Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs. Acs Medicinal Chemistry Letters. 8: 925-930. PMID 28947938 DOI: 10.1021/Acsmedchemlett.7B00249 |
0.372 |
|
| 2017 |
Bollinger KA, Felts AS, Brassard CJ, Engers JL, Rodriguez AL, Weiner RL, Cho HP, Chang S, Bubser M, Jones CK, Blobaum AL, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW. Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. Acs Medicinal Chemistry Letters. 8: 919-924. PMID 28947937 DOI: 10.1021/Acsmedchemlett.7B00279 |
0.398 |
|
| 2017 |
Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core. Bioorganic & Medicinal Chemistry Letters. PMID 28866269 DOI: 10.1016/J.Bmcl.2017.08.043 |
0.35 |
|
| 2017 |
Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW. Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 28633897 DOI: 10.1016/J.Bmcl.2017.05.042 |
0.443 |
|
| 2017 |
Felts AS, Rodriguez AL, Blobaum AL, Morrison RD, Bates BS, Thompson Gray A, Rook JM, Tantawy MN, Byers FW, Chang S, Venable DF, Luscombe VB, Tamagnan GD, Niswender CM, Daniels JS, et al. Discovery of N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A novel negative allosteric modulator of metabotropic glutamate receptor subtype 5 selected for clinical evaluation. Journal of Medicinal Chemistry. PMID 28530802 DOI: 10.1021/Acs.Jmedchem.7B00410 |
0.483 |
|
| 2017 |
Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, et al. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. Bioorganic & Medicinal Chemistry Letters. PMID 28522253 DOI: 10.1016/J.Bmcl.2017.05.014 |
0.409 |
|
| 2017 |
Wood MR, Noetzel MJ, Melancon BJ, Poslusney MS, Nance KD, Hurtado MA, Luscombe VB, Weiner RL, Rodriguez AL, Lamsal A, Chang S, Bubser M, Blobaum AL, Engers DW, Niswender CM, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. Acs Medicinal Chemistry Letters. 8: 233-238. PMID 28197318 DOI: 10.1021/Acsmedchemlett.6B00461 |
0.41 |
|
| 2016 |
Wood MR, Noetzel MJ, Tarr JC, Rodriguez AL, Lamsal A, Chang S, Foster JJ, Smith E, Chase P, Hodder PS, Engers DW, Niswender CM, Brandon NJ, Wood MW, Duggan ME, et al. Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. Bioorganic & Medicinal Chemistry Letters. PMID 27476142 DOI: 10.1016/J.Bmcl.2016.07.042 |
0.384 |
|
| 2016 |
Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ. Development and antiparkinsonian activity of VU0418506, a selective positive allosteric modulator of metabotropic glutamate receptor 4 homomers without activity at mGlu2/4 heteromers. Acs Chemical Neuroscience. PMID 27441572 DOI: 10.1021/Acschemneuro.6B00036 |
0.483 |
|
| 2016 |
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Bioorganic & Medicinal Chemistry Letters. PMID 27234146 DOI: 10.1016/J.Bmcl.2016.05.029 |
0.418 |
|
| 2016 |
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorganic & Medicinal Chemistry Letters. PMID 26988308 DOI: 10.1016/J.Bmcl.2016.03.026 |
0.486 |
|
| 2015 |
Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Design of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as selective negative allosteric modulators of metabotropic glutamate receptor subtype 2. Journal of Medicinal Chemistry. PMID 26524606 DOI: 10.1021/Acs.Jmedchem.5B01371 |
0.516 |
|
| 2015 |
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. Journal of Medicinal Chemistry. 58: 7485-500. PMID 26335039 DOI: 10.1021/Acs.Jmedchem.5B01005 |
0.463 |
|
| 2015 |
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, et al. Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 26315507 DOI: 10.1038/Npp.2015.265 |
0.34 |
|
| 2014 |
Cho HP, Garcia-Barrantes PM, Brogan JT, Hopkins CR, Niswender CM, Rodriguez AL, Venable DF, Morrison RD, Bubser M, Daniels JS, Jones CK, Conn PJ, Lindsley CW. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. Acs Chemical Biology. 9: 2334-46. PMID 25137254 DOI: 10.1021/Cb500560H |
0.427 |
|
| 2014 |
Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 24: 3307-14. PMID 24969015 DOI: 10.1016/j.bmcl.2014.06.003 |
0.352 |
|
| 2014 |
Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. 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 Chemical Neuroscience. 5: 597-610. PMID 24798819 DOI: 10.1021/Cn5000343 |
0.475 |
|
| 2013 |
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 23: 5779-85. PMID 24074843 DOI: 10.1016/J.Bmcl.2013.09.001 |
0.454 |
|
| 2013 |
Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. Bioorganic & Medicinal Chemistry Letters. 23: 5091-6. PMID 23932792 DOI: 10.1016/J.Bmcl.2013.07.029 |
0.43 |
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| 2013 |
Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorganic & Medicinal Chemistry Letters. 23: 3713-8. PMID 23727046 DOI: 10.1016/J.Bmcl.2013.05.020 |
0.408 |
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| 2013 |
Le U, Melancon BJ, Bridges TM, Vinson PN, Utley TJ, Lamsal A, Rodriguez AL, Venable D, Sheffler DJ, Jones CK, Blobaum AL, Wood MR, Daniels JS, Conn PJ, Niswender CM, et al. Discovery of a selective Mâ‚„ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorganic & Medicinal Chemistry Letters. 23: 346-50. PMID 23177787 DOI: 10.1016/J.Bmcl.2012.10.073 |
0.473 |
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| 2013 |
D'Amore V, Santolini I, van Rijn CM, Biagioni F, Molinaro G, Prete A, Conn PJ, Lindsley CW, Zhou Y, Vinson PN, Rodriguez AL, Jones CK, Stauffer SR, Nicoletti F, van Luijtelaar G, et al. Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats. Neuropharmacology. 66: 330-8. PMID 22705340 DOI: 10.1016/J.Neuropharm.2012.05.044 |
0.418 |
|
| 2012 |
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, et al. Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. Bioorganic & Medicinal Chemistry Letters. 22: 7388-92. PMID 23142615 DOI: 10.1016/J.Bmcl.2012.10.068 |
0.435 |
|
| 2012 |
Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ. Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Molecular Pharmacology. 82: 860-75. PMID 22863693 DOI: 10.1124/Mol.112.080531 |
0.519 |
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| 2012 |
Morrison RD, Blobaum AL, Byers FW, Santomango TS, Bridges TM, Stec D, Brewer KA, Sanchez-Ponce R, Corlew MM, Rush R, Felts AS, Manka J, Bates BS, Venable DF, Rodriguez AL, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 40: 1834-45. PMID 22711749 DOI: 10.1124/Dmd.112.046136 |
0.381 |
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| 2012 |
Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, et al. Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound. Chemmedchem. 7: 406-14. PMID 22267125 DOI: 10.1002/Cmdc.201100510 |
0.415 |
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| 2012 |
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, et al. Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Molecular Pharmacology. 81: 120-33. PMID 22021324 DOI: 10.1124/Mol.111.075184 |
0.455 |
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| 2012 |
Alagille D, DaCosta H, Chen Y, Hemstapat K, Rodriguez A, Baldwin RM, Jeffrey Conn P, Tamagnan GD. Erratum to “Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series” [Bioorg. Med. Chem. Lett. 21 (2011) 3243–3247] Bioorganic & Medicinal Chemistry Letters. 22: 2130. DOI: 10.1016/J.Bmcl.2012.01.054 |
0.372 |
|
| 2011 |
Lindsley CW, Bates BS, Menon UN, Jadhav SB, Kane AS, Jones CK, Rodriguez AL, Conn PJ, Olsen CM, Winder DG, Emmitte KA. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction. Acs Chemical Neuroscience. 2: 471-482. PMID 21927650 DOI: 10.1021/Cn100099N |
0.485 |
|
| 2011 |
Alagille D, DaCosta H, Chen Y, Hemstapat K, Rodriguez A, Baldwin RM, Conn PJ, Conn JP, Tamagnan GD. Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. Bioorganic & Medicinal Chemistry Letters. 21: 3243-7. PMID 21546249 DOI: 10.1016/J.Bmcl.2011.04.047 |
0.393 |
|
| 2011 |
Williams R, Manka JT, Rodriguez AL, Vinson PN, Niswender CM, Weaver CD, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Bioorganic & Medicinal Chemistry Letters. 21: 1350-3. PMID 21315585 DOI: 10.1016/J.Bmcl.2011.01.044 |
0.453 |
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| 2011 |
Zou MF, Cao J, Rodriguez AL, Conn PJ, Newman AH. Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. 21: 2650-4. PMID 21295978 DOI: 10.1016/J.Bmcl.2010.12.110 |
0.49 |
|
| 2011 |
Lamb JP, Engers DW, Niswender CM, Rodriguez AL, Venable DF, Conn PJ, Lindsley CW. Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. Bioorganic & Medicinal Chemistry Letters. 21: 2711-4. PMID 21183344 DOI: 10.1016/J.Bmcl.2010.11.119 |
0.415 |
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| 2010 |
Zhou Y, Manka JT, Rodriguez AL, Weaver CD, Days EL, Vinson PN, Jadhav S, Hermann EJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. Acs Medicinal Chemistry Letters. 1: 433-438. PMID 23308336 DOI: 10.1021/Ml100181A |
0.46 |
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| 2010 |
Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. Acs Chemical Neuroscience. 1: 702-716. PMID 20981342 DOI: 10.1021/Cn100051M |
0.5 |
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| 2010 |
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, et al. 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. Molecular Pharmacology. 78: 1105-23. PMID 20923853 DOI: 10.1124/Mol.110.067207 |
0.501 |
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| 2010 |
Lowe EW, Ferrebee A, Rodriguez AL, Conn PJ, Meiler J. 3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. 20: 5922-4. PMID 20732812 DOI: 10.1016/J.Bmcl.2010.07.061 |
0.385 |
|
| 2010 |
Felts AS, Lindsley SR, Lamb JP, Rodriguez AL, Menon UN, Jadhav S, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats. Bioorganic & Medicinal Chemistry Letters. 20: 4390-4. PMID 20598884 DOI: 10.1016/J.Bmcl.2010.06.064 |
0.422 |
|
| 2010 |
Mueller R, Rodriguez AL, Dawson ES, Butkiewicz M, Nguyen TT, Oleszkiewicz S, Bleckmann A, Weaver CD, Lindsley CW, Conn PJ, Meiler J. Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening. Acs Chemical Neuroscience. 1: 288-305. PMID 20414370 DOI: 10.1021/Cn9000389 |
0.425 |
|
| 2010 |
Zhang P, Zou MF, Rodriguez AL, Conn PJ, Newman AH. Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry. 18: 3026-35. PMID 20382541 DOI: 10.1016/J.Bmc.2010.03.053 |
0.496 |
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| 2009 |
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. Bioorganic & Medicinal Chemistry Letters. 19: 6502-6. PMID 19875287 DOI: 10.1016/J.Bmcl.2009.10.059 |
0.355 |
|
| 2009 |
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. Bioorganic & Medicinal Chemistry Letters. 19: 6623-6. PMID 19854049 DOI: 10.1016/J.Bmcl.2009.10.024 |
0.509 |
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| 2009 |
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. Journal of Medicinal Chemistry. 52: 4103-6. PMID 19537763 DOI: 10.1021/Jm900654C |
0.502 |
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| 2009 |
Kulkarni SS, Zou MF, Cao J, Deschamps JR, Rodriguez AL, Conn PJ, Newman AH. Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. Journal of Medicinal Chemistry. 52: 3563-75. PMID 19445453 DOI: 10.1021/Jm900172F |
0.477 |
|
| 2009 |
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. Bioorganic & Medicinal Chemistry Letters. 19: 3209-13. PMID 19443219 DOI: 10.1016/J.Bmcl.2009.04.110 |
0.423 |
|
| 2009 |
Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. Chemmedchem. 4: 505-11. PMID 19197923 DOI: 10.1002/Cmdc.200800357 |
0.402 |
|
| 2009 |
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, et al. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Molecular Pharmacology. 75: 577-88. PMID 19047481 DOI: 10.1124/Mol.108.052886 |
0.493 |
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| 2008 |
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, et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Molecular Pharmacology. 74: 1345-58. PMID 18664603 DOI: 10.1124/Mol.108.049551 |
0.444 |
|
| 2008 |
Sharma S, Rodriguez AL, Conn PJ, Lindsley CW. Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorganic & Medicinal Chemistry Letters. 18: 4098-101. PMID 18550372 DOI: 10.1016/J.Bmcl.2008.05.091 |
0.458 |
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| 2008 |
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. Nature Chemical Biology. 4: 42-50. PMID 18059262 DOI: 10.1038/Nchembio.2007.55 |
0.432 |
|
| 2007 |
Rodriguez AL, Williams R. Recent progress in the development of allosteric modulators of mGluR5. Current Opinion in Drug Discovery & Development. 10: 715-22. PMID 17987523 |
0.353 |
|
| 2005 |
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ. 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. Molecular Pharmacology. 68: 1793-802. PMID 16155210 DOI: 10.1124/Mol.105.016139 |
0.528 |
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| 2005 |
Zhang Y, Rodriguez AL, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. The Journal of Pharmacology and Experimental Therapeutics. 315: 1212-9. PMID 16135701 DOI: 10.1124/Jpet.105.090308 |
0.317 |
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| 2005 |
Galici R, Echemendia NG, Rodriguez AL, Conn PJ. A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity. The Journal of Pharmacology and Experimental Therapeutics. 315: 1181-7. PMID 16123306 DOI: 10.1124/Jpet.105.091074 |
0.486 |
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| 2005 |
Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y. Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology. 49: 57-69. PMID 15993439 DOI: 10.1016/J.Neuropharm.2005.03.006 |
0.346 |
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| 2005 |
Tamrazi A, Carlson KE, Rodriguez AL, Katzenellenbogen JA. Coactivator proteins as determinants of estrogen receptor structure and function: spectroscopic evidence for a novel coactivator-stabilized receptor conformation. Molecular Endocrinology (Baltimore, Md.). 19: 1516-28. PMID 15661830 DOI: 10.1210/Me.2004-0458 |
0.753 |
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| 2004 |
Nettles KW, Sun J, Radek JT, Sheng S, Rodriguez AL, Katzenellenbogen JA, Katzenellenbogen BS, Greene GL. Allosteric Control of Ligand Selectivity between Estrogen Receptors α and β: Implications for Other Nuclear Receptors Molecular Cell. 13: 317-327. PMID 14967140 DOI: 10.1016/S1097-2765(04)00054-1 |
0.616 |
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| 2004 |
Rodriguez AL, Tamrazi A, Collins ML, Katzenellenbogen JA. Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding. Journal of Medicinal Chemistry. 47: 600-11. PMID 14736241 DOI: 10.1021/Jm030404C |
0.753 |
|
| 2002 |
Nishiguchi GA, Rodriguez AL, Katzenellenbogen JA. Diaryl-dialkyl-substituted pyrazoles: regioselective synthesis and binding affinity for the estrogen receptor. Bioorganic & Medicinal Chemistry Letters. 12: 947-50. PMID 11959000 DOI: 10.1016/S0960-894X(02)00057-4 |
0.621 |
|
| 2002 |
Mull ES, Sattigeri VJ, Rodriguez AL, Katzenellenbogen JA. Aryl cyclopentadienyl tricarbonyl rhenium complexes: novel ligands for the estrogen receptor with potential use as estrogen radiopharmaceuticals. Bioorganic & Medicinal Chemistry. 10: 1381-98. PMID 11886802 DOI: 10.1016/S0968-0896(01)00406-0 |
0.605 |
|
| 2001 |
Mortensen DS, Rodriguez AL, Carlson KE, Sun J, Katzenellenbogen BS, Katzenellenbogen JA. Synthesis and biological evaluation of a novel series of furans: ligands selective for estrogen receptor alpha. Journal of Medicinal Chemistry. 44: 3838-48. PMID 11689070 DOI: 10.1021/Jm010211U |
0.755 |
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| 2001 |
Mortensen DS, Rodriguez AL, Sun J, Katzenellenbogen BS, Katzenellenbogen JA. Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha. Bioorganic & Medicinal Chemistry Letters. 11: 2521-4. PMID 11549460 DOI: 10.1016/S0960-894X(01)00488-7 |
0.759 |
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