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Items: 1 to 50 of 82

1.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

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, Emmitte KA, Jones CK, Blobaum AL, Jeffrey Conn P, Niswender CM, Hopkins CR, Lindsley CW.

Bioorg Med Chem Lett. 2018 Nov 1. pii: S0960-894X(18)30853-9. doi: 10.1016/j.bmcl.2018.10.050. [Epub ahead of print]

PMID:
30503632
2.

Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.

Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI.

J Med Chem. 2018 Nov 30. doi: 10.1021/acs.jmedchem.8b01671. [Epub ahead of print]

PMID:
30451500
3.

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

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.

Bioorg Med Chem Lett. 2018 Nov 10. pii: S0960-894X(18)30882-5. doi: 10.1016/j.bmcl.2018.11.017. [Epub ahead of print]

PMID:
30446311
4.

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

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.

J Med Chem. 2018 Oct 31. doi: 10.1021/acs.jmedchem.8b01266. [Epub ahead of print]

PMID:
30350962
5.

VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events.

Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW.

ACS Med Chem Lett. 2018 Sep 4;9(9):917-922. doi: 10.1021/acsmedchemlett.8b00261. eCollection 2018 Sep 13.

PMID:
30258541
6.

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).

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.

J Med Chem. 2018 Sep 24. doi: 10.1021/acs.jmedchem.8b00994. [Epub ahead of print]

PMID:
30247901
7.

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.

Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ.

Mol Psychiatry. 2018 Aug 16. doi: 10.1038/s41380-018-0206-2. [Epub ahead of print]

PMID:
30116027
8.

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators.

Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Lingenfelter KS, Luscombe VB, Han C, Melancon BJ, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Aug 9. doi: 10.1021/acschemneuro.8b00311. [Epub ahead of print]

PMID:
30086237
9.

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.

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, Hopkins CR.

Bioorg Med Chem Lett. 2018 Aug 15;28(15):2641-2646. doi: 10.1016/j.bmcl.2018.06.034. Epub 2018 Jun 19.

PMID:
29958762
10.

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.

Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12.

PMID:
29895592
11.

Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.

Friggeri L, Hargrove TY, Wawrzak Z, Blobaum AL, Rachakonda G, Lindsley CW, Villalta F, Nes WD, Botta M, Guengerich FP, Lepesheva GI.

J Med Chem. 2018 Jul 12;61(13):5679-5691. doi: 10.1021/acs.jmedchem.8b00641. Epub 2018 Jun 25.

PMID:
29894182
12.

The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.

Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2175-2179. doi: 10.1016/j.bmcl.2018.05.009. Epub 2018 May 5.

PMID:
29754948
13.

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1679-1685. doi: 10.1016/j.bmcl.2018.04.053. Epub 2018 Apr 22.

PMID:
29705142
14.

A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.

Rook JM, Bertron JL, Cho HP, Garcia-Barrantes PM, Moran SP, Maksymetz JT, Nance KD, Dickerson JW, Remke DH, Chang S, Harp JM, Blobaum AL, Niswender CM, Jones CK, Stauffer SR, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Sep 19;9(9):2274-2285. doi: 10.1021/acschemneuro.8b00131. Epub 2018 May 8.

PMID:
29701957
15.

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

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, Lindsley CW.

ACS Med Chem Lett. 2017 Nov 8;8(12):1326-1330. doi: 10.1021/acsmedchemlett.7b00429. eCollection 2017 Dec 14.

PMID:
29259756
16.

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

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, Niswender CM, Lindsley CW.

ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115. doi: 10.1021/acsmedchemlett.7b00317. eCollection 2017 Oct 12.

17.

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.

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.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4858-4866. doi: 10.1016/j.bmcl.2017.09.042. Epub 2017 Sep 20.

18.

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs.

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, Emmitte KA, Lindsley CW.

ACS Med Chem Lett. 2017 Aug 15;8(9):925-930. doi: 10.1021/acsmedchemlett.7b00249. eCollection 2017 Sep 14.

19.

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core.

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.

ACS Med Chem Lett. 2017 Aug 3;8(9):919-924. doi: 10.1021/acsmedchemlett.7b00279. eCollection 2017 Sep 14.

20.

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

Crouch RD, Blobaum AL, Felts AS, Conn PJ, Lindsley CW.

Drug Metab Dispos. 2017 Dec;45(12):1245-1259. doi: 10.1124/dmd.117.077552. Epub 2017 Sep 22.

21.

mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

Gogliotti RG, Senter RK, Fisher NM, Adams J, Zamorano R, Walker AG, Blobaum AL, Engers DW, Hopkins CR, Daniels JS, Jones CK, Lindsley CW, Xiang Z, Conn PJ, Niswender CM.

Sci Transl Med. 2017 Aug 16;9(403). pii: eaai7459. doi: 10.1126/scitranslmed.aai7459.

22.

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.

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, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

J Med Chem. 2017 Jun 22;60(12):5072-5085. doi: 10.1021/acs.jmedchem.7b00410. Epub 2017 May 31.

23.

Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain.

Li Z, Tseng PY, Tiwari V, Xu Q, He SQ, Wang Y, Zheng Q, Han L, Wu Z, Blobaum AL, Cui Y, Tiwari V, Sun S, Cheng Y, Huang-Lionnet JH, Geng Y, Xiao B, Peng J, Hopkins C, Raja SN, Guan Y, Dong X.

Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):E1996-E2005. doi: 10.1073/pnas.1615255114. Epub 2017 Feb 21.

24.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

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, Jones CK, Brandon NJ, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

ACS Med Chem Lett. 2016 Dec 16;8(2):233-238. doi: 10.1021/acsmedchemlett.6b00461. eCollection 2017 Feb 9.

25.

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW.

J Med Chem. 2017 Feb 23;60(4):1611-1616. doi: 10.1021/acs.jmedchem.6b01706. Epub 2017 Feb 3.

PMID:
28103022
26.

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.

Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2017 Apr 19;8(4):866-883. doi: 10.1021/acschemneuro.6b00429. Epub 2017 Jan 10.

27.

Contributions of Protease-Activated Receptors PAR1 and PAR4 to Thrombin-Induced GPIIbIIIa Activation in Human Platelets.

Duvernay MT, Temple KJ, Maeng JG, Blobaum AL, Stauffer SR, Lindsley CW, Hamm HE.

Mol Pharmacol. 2017 Jan;91(1):39-47. Epub 2016 Oct 26.

28.

Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.

Temple KJ, Duvernay MT, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5481-5486. doi: 10.1016/j.bmcl.2016.10.020. Epub 2016 Oct 11.

29.

Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

Grannan MD, Mielnik CA, Moran SP, Gould RW, Ball J, Lu Z, Bubser M, Ramsey AJ, Abe M, Cho HP, Nance KD, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW, Jones CK.

ACS Chem Neurosci. 2016 Dec 21;7(12):1706-1716. doi: 10.1021/acschemneuro.6b00230. Epub 2016 Oct 5.

30.

Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound.

Bertron JL, Ennis EA, Tarr CJ, Wright J, Dickerson JW, Locuson CW, Blobaum AL, Rook JM, Blakely RD, Lindsley CW.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4637-4640. doi: 10.1016/j.bmcl.2016.08.062. Epub 2016 Aug 21.

PMID:
27575469
31.

Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin.

Temple KJ, Duvernay MT, Young SE, Wen W, Wu W, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW.

J Med Chem. 2016 Aug 25;59(16):7690-5. doi: 10.1021/acs.jmedchem.6b00928. Epub 2016 Aug 8.

32.

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.

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.

ACS Chem Neurosci. 2016 Sep 21;7(9):1201-11. doi: 10.1021/acschemneuro.6b00036. Epub 2016 Aug 5.

33.

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):2984-2987. doi: 10.1016/j.bmcl.2016.05.029. Epub 2016 May 11.

34.

ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels.

Swale DR, Kurata H, Kharade SV, Sheehan J, Raphemot R, Voigtritter KR, Figueroa EE, Meiler J, Blobaum AL, Lindsley CW, Hopkins CR, Denton JS.

ACS Chem Neurosci. 2016 Jul 20;7(7):1013-23. doi: 10.1021/acschemneuro.6b00111. Epub 2016 May 24.

35.

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.

Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3822-5. doi: 10.1016/j.bmcl.2016.04.083. Epub 2016 Apr 29.

36.

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.

Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2915-2919. doi: 10.1016/j.bmcl.2016.04.041. Epub 2016 Apr 19.

37.

Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.

Witt JO, McCollum AL, Hurtado MA, Huseman ED, Jeffries DE, Temple KJ, Plumley HC, Blobaum AL, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2016 May 15;26(10):2481-2488. doi: 10.1016/j.bmcl.2016.03.102. Epub 2016 Mar 30.

38.

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

ACS Chem Neurosci. 2016 Sep 21;7(9):1192-200. doi: 10.1021/acschemneuro.6b00035. Epub 2016 May 3.

39.

Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Garcia-Barrantes PM, Cho HP, Starr TM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 May 1;26(9):2289-92. doi: 10.1016/j.bmcl.2016.03.044. Epub 2016 Mar 14.

40.

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.

Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1894-900. doi: 10.1016/j.bmcl.2016.03.026. Epub 2016 Mar 9.

41.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.

Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1869-72. doi: 10.1016/j.bmcl.2016.03.031. Epub 2016 Mar 10.

42.

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):751-756. doi: 10.1016/j.bmcl.2015.12.104. Epub 2016 Jan 2.

43.

Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists.

Jeffries DE, Witt JO, McCollum AL, Temple KJ, Hurtado MA, Harp JM, Blobaum AL, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5757-5764. doi: 10.1016/j.bmcl.2016.10.049. Epub 2016 Oct 17.

PMID:
28327307
44.

Conservative Secondary Shell Substitution In Cyclooxygenase-2 Reduces Inhibition by Indomethacin Amides and Esters via Altered Enzyme Dynamics.

Konkle ME, Blobaum AL, Moth CW, Prusakiewicz JJ, Xu S, Ghebreselasie K, Akingbade D, Jacobs AT, Rouzer CA, Lybrand TP, Marnett LJ.

Biochemistry. 2016 Jan 19;55(2):348-59. doi: 10.1021/acs.biochem.5b01222. Epub 2015 Dec 31.

45.

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

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.

J Med Chem. 2015 Nov 25;58(22):9027-40. doi: 10.1021/acs.jmedchem.5b01371. Epub 2015 Nov 11.

46.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5107-10. doi: 10.1016/j.bmcl.2015.10.013. Epub 2015 Oct 9.

47.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW.

J Med Chem. 2015 Oct 22;58(20):7959-71. doi: 10.1021/acs.jmedchem.5b00727. Epub 2015 Oct 8.

48.

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.

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, Emmitte KA.

J Med Chem. 2015 Sep 24;58(18):7485-500. doi: 10.1021/acs.jmedchem.5b01005. Epub 2015 Sep 10.

49.

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.

Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS.

Drug Metab Dispos. 2015 Nov;43(11):1718-26. doi: 10.1124/dmd.115.064006. Epub 2015 Aug 11.

50.

The discovery and characterization of a centrally penetrant (ML396) and a peripherally restricted (ML397) pan-Group III mGlu positive allosteric modulators.

Jalan-Sakrikar N, Roper-Field J, Klar R, Mattman M, Walker AG, Zamorano R, Xiang Z, Byers CF, Blobaum AL, Engers D, Weaver CD, Days E, Utley TJ, Melancon B, Daniels JS, Wood MR, Lindsley CW, Conn PJ, Hopkins CR, Niswender CM.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2014 Apr 15 [updated 2015 Jan 16].

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