| Year |
Citation |
Score |
| 2023 |
Jörg M, van der Westhuizen ET, Lu Y, Christopher Choy KH, Shackleford DM, Khajehali E, Tobin AB, Thal DM, Capuano B, Christopoulos A, Valant C, Scammells PJ. Design, synthesis and evaluation of novel 2-phenyl-3-(1H-pyrazol-4-yl)pyridine positive allosteric modulators for the M mAChR. European Journal of Medicinal Chemistry. 258: 115588. PMID 37423123 DOI: 10.1016/j.ejmech.2023.115588 |
0.394 |
|
| 2022 |
Calic PPS, Vinh NB, Webb CT, Malcolm TR, Ngo A, Lowes K, Drinkwater N, McGowan S, Scammells PJ. Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation. European Journal of Medicinal Chemistry. 248: 115051. PMID 36634455 DOI: 10.1016/j.ejmech.2022.115051 |
0.329 |
|
| 2022 |
Awalt JK, Nguyen ATN, Fyfe TJ, Thai BS, White PJ, Christopoulos A, Jörg M, May LT, Scammells PJ. Examining the Role of the Linker in Bitopic -Substituted Adenosine Derivatives Acting as Biased Adenosine A Receptor Agonists. Journal of Medicinal Chemistry. PMID 35729775 DOI: 10.1021/acs.jmedchem.2c00320 |
0.338 |
|
| 2022 |
Wakeham MCL, Davie BJ, Chalmers DK, Christopoulos A, Capuano B, Valant C, Scammells PJ. Structural Features of Iperoxo-BQCA Muscarinic Acetylcholine Receptor Hybrid Ligands Determining Subtype Selectivity and Efficacy. Acs Chemical Neuroscience. 13: 97-111. PMID 34905693 DOI: 10.1021/acschemneuro.1c00572 |
0.348 |
|
| 2021 |
Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, ... ... Scammells P, et al. Positive allosteric mechanisms of adenosine A receptor-mediated analgesia. Nature. PMID 34497422 DOI: 10.1038/s41586-021-03897-2 |
0.312 |
|
| 2021 |
Fyfe TJ, Scammells PJ, Lane JR, Capuano B. Enantioenriched Positive Allosteric Modulators Display Distinct Pharmacology at the Dopamine D Receptor. Molecules (Basel, Switzerland). 26. PMID 34206465 DOI: 10.3390/molecules26133799 |
0.745 |
|
| 2021 |
Comeo E, Trinh P, Nguyen AT, Nowell CJ, Kindon ND, Soave M, Stoddart LA, White JM, Hill SJ, Kellam B, Halls ML, May LT, Scammells PJ. Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A Receptor in Living Cells. Journal of Medicinal Chemistry. PMID 33724031 DOI: 10.1021/acs.jmedchem.0c02067 |
0.684 |
|
| 2020 |
Scammells PJ, Jörg M, Khajehali E, van der Westhuizen ET, Choy KHC, Shackleford D, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A. Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. Chemmedchem. PMID 32851779 DOI: 10.1002/cmdc.202000540 |
0.436 |
|
| 2019 |
Comeo E, Kindon ND, Soave M, Stoddart LA, Kilpatrick L, Scammells PJ, Hill SJ, Kellam B. Subtype-selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor. Journal of Medicinal Chemistry. PMID 31887252 DOI: 10.1021/Acs.Jmedchem.9B01856 |
0.7 |
|
| 2019 |
Cooper SL, March J, Sabbatini AR, Hill SJ, Jörg M, Scammells PJ, Woolard J. The effect of two selective A -receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats. British Journal of Pharmacology. PMID 31596949 DOI: 10.1111/Bph.14870 |
0.514 |
|
| 2019 |
Fyfe TJ, Kellam B, Sykes DA, Capuano B, Scammells PJ, Lane JR, Charlton SJ, Mistry SN. Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D Receptor. Journal of Medicinal Chemistry. PMID 31580666 DOI: 10.1021/Acs.Jmedchem.9B00864 |
0.759 |
|
| 2019 |
Klein Herenbrink C, Verma R, Lim HD, Kopinathan A, Keen A, Shonberg J, Draper-Joyce CJ, Scammells PJ, Christopoulos A, Javitch JA, Capuano B, Shi L, Lane JR. Molecular determinants of the intrinsic efficacy of the antipsychotic aripiprazole. Acs Chemical Biology. PMID 31339684 DOI: 10.1021/Acschembio.9B00342 |
0.376 |
|
| 2019 |
Hollingsworth SA, Kelly B, Valant C, Michaelis JA, Mastromihalis O, Thompson G, Venkatakrishnan AJ, Hertig S, Scammells PJ, Sexton PM, Felder CC, Christopoulos A, Dror RO. Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs. Nature Communications. 10: 3289. PMID 31337749 DOI: 10.1038/s41467-019-11062-7 |
0.436 |
|
| 2019 |
Fyfe TJ, Kellam B, Mistry SN, Scammells PJ, Lane JR, Capuano B. Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D receptor. European Journal of Medicinal Chemistry. 168: 474-490. PMID 30849613 DOI: 10.1016/J.Ejmech.2019.01.061 |
0.771 |
|
| 2019 |
Cooper SL, Soave M, Jörg M, Scammells PJ, Woolard J, Hill SJ. Probe dependence of allosteric enhancers on the binding affinity of adenosine A -receptor agonists at rat and human A -receptors measured using NanoBRET. British Journal of Pharmacology. PMID 30644086 DOI: 10.1111/Bph.14575 |
0.536 |
|
| 2018 |
Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ. 6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity. Acs Chemical Neuroscience. PMID 30547573 DOI: 10.1021/acschemneuro.8b00613 |
0.464 |
|
| 2018 |
Vinh NB, Drinkwater N, Malcolm TR, Kassiou M, Lucantoni L, Grin PM, Butler GS, Duffy S, Overall CM, Avery VM, Scammells PJ, McGowan S. Hydroxamic acid inhibitors provide cross-species inhibition of Plasmodium M1 and M17 aminopeptidases. Journal of Medicinal Chemistry. PMID 30537832 DOI: 10.1021/Acs.Jmedchem.8B01310 |
0.308 |
|
| 2018 |
Kopinathan A, Draper-Joyce CJ, Szabo M, Scammells PJ, Lane JR, Capuano B. Subtle modifications to the indole-2-carboxamide motif of the negative allosteric modulator N-(( trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) yield dramatic changes in pharmacological activity at the dopamine D receptor. Journal of Medicinal Chemistry. PMID 29890071 DOI: 10.1021/acs.jmedchem.8b00192 |
0.432 |
|
| 2018 |
Khajehali E, Valant C, Jörg M, Tobin AB, Jeffrey Conn P, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A. Probing the binding site of novel selective positive allosteric modulators at the M mAChR. Biochemical Pharmacology. PMID 29777683 DOI: 10.1016/J.Bcp.2018.05.009 |
0.384 |
|
| 2018 |
van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A. Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M Muscarinic Acetylcholine Receptors. Molecular Pharmacology. 94: 770-783. PMID 29691279 DOI: 10.1124/mol.118.111633 |
0.76 |
|
| 2018 |
Fyfe TJ, Zarzycka B, Lim HD, Kellam B, Mistry SN, Katritch V, Scammells PJ, Lane JR, Capuano B. A Thieno[2,3-d]pyrimidine Scaffold is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor. Journal of Medicinal Chemistry. PMID 29683325 DOI: 10.1021/Acs.Jmedchem.7B01565 |
0.776 |
|
| 2018 |
Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ. Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles. Journal of Medicinal Chemistry. 61: 2875-2894. PMID 29544056 DOI: 10.1021/acs.jmedchem.7b01812 |
0.46 |
|
| 2018 |
Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions. Scientific Reports. 8: 1208. PMID 29352161 DOI: 10.1038/S41598-018-19642-1 |
0.36 |
|
| 2018 |
Draper-Joyce CJ, Michino M, Verma RK, Herenbrink CK, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor. Biochemical Pharmacology. PMID 29325769 DOI: 10.1016/J.Bcp.2018.01.002 |
0.394 |
|
| 2018 |
Lam R, Gondin AB, Canals M, Kellam B, Briddon SJ, Graham B, Scammells PJ. Fluorescently Labelled Morphine Derivatives for Bioimaging Studies. Journal of Medicinal Chemistry. PMID 29291353 DOI: 10.1021/Acs.Jmedchem.7B01811 |
0.597 |
|
| 2017 |
Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A. Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity. Cell. 168: 867-877.e13. PMID 28235198 DOI: 10.1016/j.cell.2017.01.042 |
0.306 |
|
| 2017 |
Awalt JK, Lam R, Kellam B, Graham B, Scammells PJ, Singer RD. Utility of iron nanoparticles and a solution-phase iron species for the N-demethylation of alkaloids Green Chemistry. 19: 2587-2594. DOI: 10.1039/C7Gc00436B |
0.521 |
|
| 2016 |
Jörg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ. Novel Irreversible Agonists Acting at the A1 Adenosine Receptor. Journal of Medicinal Chemistry. PMID 27958734 DOI: 10.1021/acs.jmedchem.6b01561 |
0.38 |
|
| 2016 |
Choy KH, Shackleford DM, Malone DT, Mistry SN, Patil RT, Scammells PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A. Positive allosteric modulation of the muscarinic M1 receptor improves efficacy of antipsychotics in mouse glutamatergic deficit models of behavior. The Journal of Pharmacology and Experimental Therapeutics. PMID 27630144 DOI: 10.1124/Jpet.116.235788 |
0.733 |
|
| 2016 |
Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT. The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. Biochemical Pharmacology. PMID 27520486 DOI: 10.1016/j.bcp.2016.08.007 |
0.325 |
|
| 2016 |
Kopinathan A, Scammells PJ, Lane JR, Capuano B. Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology. Future Medicinal Chemistry. PMID 27357619 DOI: 10.4155/fmc-2016-0010 |
0.398 |
|
| 2016 |
Jörg M, Scammells PJ. Guidelines for the Synthesis of Small-Molecule Irreversible Probes Targeting G Protein-Coupled Receptors. Chemmedchem. 11: 1488-98. PMID 27347648 DOI: 10.1002/cmdc.201600066 |
0.326 |
|
| 2016 |
Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR. The role of kinetic context in apparent biased agonism at GPCRs. Nature Communications. 7: 10842. PMID 26905976 DOI: 10.1038/Ncomms10842 |
0.366 |
|
| 2016 |
Mistry SN, Lim H, Jörg M, Capuano B, Christopoulos A, Lane JR, Scammells PJ. Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 26891194 DOI: 10.1021/Acschemneuro.6B00018 |
0.759 |
|
| 2016 |
Drinkwater N, Vinh NB, Mistry SN, Bamert RS, Ruggeri C, Holleran JP, Loganathan S, Paiardini A, Charman SA, Powell AK, Avery VM, McGowan S, Scammells PJ. Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions. European Journal of Medicinal Chemistry. 110: 43-64. PMID 26807544 DOI: 10.1016/J.Ejmech.2016.01.015 |
0.719 |
|
| 2015 |
Schembri LS, Stoddart LA, Briddon SJ, Kellam B, Canals M, Graham B, Scammells PJ. Synthesis, Biological Evaluation and Utility of Fluorescent Ligands Targeting the µ-Opioid Receptor. Journal of Medicinal Chemistry. PMID 26632862 DOI: 10.1021/Acs.Jmedchem.5B01664 |
0.623 |
|
| 2015 |
Mistry SN, Jörg M, Lim H, Vinh NB, Sexton PM, Capuano B, Christopoulos A, Lane JR, Scammells PJ. 4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor. Journal of Medicinal Chemistry. PMID 26624844 DOI: 10.1021/Acs.Jmedchem.5B01562 |
0.77 |
|
| 2015 |
Mistry SN, Shonberg J, Draper-Joyce CJ, Klein Herenbrink C, Michino M, Shi L, Christopoulos A, Capuano B, Scammells PJ, Lane JR. Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand. Journal of Medicinal Chemistry. 58: 6819-43. PMID 26258690 DOI: 10.1021/Acs.Jmedchem.5B00585 |
0.757 |
|
| 2015 |
Shonberg J, Draper-Joyce C, Mistry SN, Christopoulos A, Scammells PJ, Lane JR, Capuano B. Structure-Activity Study of N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a Bitopic Ligand That Acts as a Negative Allosteric Modulator of the Dopamine D2 Receptor. Journal of Medicinal Chemistry. PMID 26052807 DOI: 10.1021/Acs.Jmedchem.5B00581 |
0.775 |
|
| 2015 |
Paiardini A, Bamert RS, Kannan-Sivaraman K, Drinkwater N, Mistry SN, Scammells PJ, McGowan S. Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18. Plos One. 10: e0115859. PMID 25700165 DOI: 10.1371/Journal.Pone.0115859 |
0.726 |
|
| 2015 |
Jörg M, May LT, Mak FS, Lee KC, Miller ND, Scammells PJ, Capuano B. Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease. Journal of Medicinal Chemistry. 58: 718-38. PMID 25490054 DOI: 10.1021/jm501254d |
0.456 |
|
| 2015 |
Cook AE, Mistry SN, Gregory KJ, Furness SG, Sexton PM, Scammells PJ, Conigrave AD, Christopoulos A, Leach K. Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics. British Journal of Pharmacology. 172: 185-200. PMID 25220431 DOI: 10.1111/Bph.12937 |
0.703 |
|
| 2015 |
Jorg M, Scammells PJ, Capuano B. The dopamine D2 and adenosine A2A receptors: past, present and future trends for the treatment of Parkinson's disease. Current Medicinal Chemistry. 21: 3188-210. PMID 24533801 DOI: 10.2174/1389200215666140217110716 |
0.378 |
|
| 2014 |
Abdul-Ridha A, Lane JR, Mistry SN, López L, Sexton PM, Scammells PJ, Christopoulos A, Canals M. Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 289: 33701-11. PMID 25326383 DOI: 10.1074/Jbc.M114.604967 |
0.77 |
|
| 2014 |
Mistry SN, Drinkwater N, Ruggeri C, Sivaraman KK, Loganathan S, Fletcher S, Drag M, Paiardini A, Avery VM, Scammells PJ, McGowan S. Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors. Journal of Medicinal Chemistry. 57: 9168-83. PMID 25299353 DOI: 10.1021/Jm501323A |
0.718 |
|
| 2014 |
Davie BJ, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor. Acs Chemical Neuroscience. 5: 902-7. PMID 25188871 DOI: 10.1021/cn500173x |
0.4 |
|
| 2014 |
Lane JR, Donthamsetti P, Shonberg J, Draper-Joyce CJ, Dentry S, Michino M, Shi L, López L, Scammells PJ, Capuano B, Sexton PM, Javitch JA, Christopoulos A. A new mechanism of allostery in a G protein-coupled receptor dimer. Nature Chemical Biology. 10: 745-52. PMID 25108820 DOI: 10.1038/Nchembio.1593 |
0.397 |
|
| 2014 |
Keov P, López L, Devine SM, Valant C, Lane JR, Scammells PJ, Sexton PM, Christopoulos A. Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 289: 23817-37. PMID 25006252 DOI: 10.1074/jbc.M114.582874 |
0.378 |
|
| 2014 |
Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M â‚ muscarinic acetylcholine receptor. Journal of Medicinal Chemistry. 57: 5405-18. PMID 24856614 DOI: 10.1021/jm500556a |
0.408 |
|
| 2014 |
Shonberg J, Lopez L, Scammells PJ, Christopoulos A, Capuano B, Lane JR. Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective. Medicinal Research Reviews. 34: 1286-330. PMID 24796277 DOI: 10.1002/med.21318 |
0.334 |
|
| 2014 |
Valant C, May LT, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A. Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proceedings of the National Academy of Sciences of the United States of America. 111: 4614-9. PMID 24619092 DOI: 10.1073/pnas.1320962111 |
0.369 |
|
| 2014 |
Jörg M, Kaczor AA, Mak FS, Lee KCK, Poso A, Miller ND, Scammells PJ, Capuano B. Investigation of novel ropinirole analogues: Synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands Medchemcomm. 5: 891-898. DOI: 10.1039/c4md00066h |
0.449 |
|
| 2013 |
Shonberg J, Herenbrink CK, López L, Christopoulos A, Scammells PJ, Capuano B, Lane JR. A structure-activity analysis of biased agonism at the dopamine D2 receptor. Journal of Medicinal Chemistry. 56: 9199-221. PMID 24138311 DOI: 10.1021/jm401318w |
0.434 |
|
| 2013 |
Keov P, Valant C, Devine SM, Lane JR, Scammells PJ, Sexton PM, Christopoulos A. Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor. Molecular Pharmacology. 84: 425-37. PMID 23798605 DOI: 10.1124/mol.113.087320 |
0.405 |
|
| 2013 |
Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. Journal of Medicinal Chemistry. 56: 5151-72. PMID 23718562 DOI: 10.1021/Jm400540B |
0.775 |
|
| 2013 |
Davie BJ, Christopoulos A, Scammells PJ. Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits. Acs Chemical Neuroscience. 4: 1026-48. PMID 23659787 DOI: 10.1021/cn400086m |
0.358 |
|
| 2013 |
Jörg M, Shonberg J, Mak FS, Miller ND, Yuriev E, Scammells PJ, Capuano B. Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space. Bioorganic & Medicinal Chemistry Letters. 23: 3427-33. PMID 23602401 DOI: 10.1016/j.bmcl.2013.03.070 |
0.38 |
|
| 2013 |
Shonberg J, Lane JR, Scammells PJ, Capuano B. Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor Medchemcomm. 4: 1290. DOI: 10.1039/C3MD00154G |
0.38 |
|
| 2013 |
Davie B, Valant C, Capuano B, Scammells P, Christopoulos A. P.1.j.011 Synthesis and pharmacological evaluation of irreversible allosteric ligands for the M1 muscarinic acetylcholine receptor European Neuropsychopharmacology. 23: S287-S288. DOI: 10.1016/S0924-977X(13)70449-8 |
0.357 |
|
| 2012 |
Gosling JI, Baker SP, Haynes JM, Kassiou M, Pouton CW, Warfe L, White PJ, Scammells PJ. Synthesis and biological evaluation of adenosines with heterobicyclic and polycyclic N(6)-substituents as adenosine A(1) receptor agonists. Chemmedchem. 7: 1191-201. PMID 22684887 DOI: 10.1002/cmdc.201200208 |
0.348 |
|
| 2012 |
Valant C, Aurelio L, Devine SM, Ashton TD, White JM, Sexton PM, Christopoulos A, Scammells PJ. Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor. Journal of Medicinal Chemistry. 55: 2367-75. PMID 22315963 DOI: 10.1021/jm201600e |
0.361 |
|
| 2012 |
Canals M, Lane JR, Wen A, Scammells PJ, Sexton PM, Christopoulos A. A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation. The Journal of Biological Chemistry. 287: 650-659. PMID 22086918 DOI: 10.1074/jbc.M111.314278 |
0.413 |
|
| 2011 |
Aurelio L, Christopoulos A, Flynn BL, Scammells PJ, Sexton PM, Valant C. The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor. Bioorganic & Medicinal Chemistry Letters. 21: 3704-7. PMID 21612922 DOI: 10.1016/j.bmcl.2011.04.080 |
0.304 |
|
| 2011 |
Shonberg J, Scammells PJ, Capuano B. Design strategies for bivalent ligands targeting GPCRs. Chemmedchem. 6: 963-74. PMID 21520422 DOI: 10.1002/Cmdc.201100101 |
0.418 |
|
| 2010 |
Aurelio L, Valant C, Flynn BL, Sexton PM, White JM, Christopoulos A, Scammells PJ. Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A(1) adenosine receptor modulation. Journal of Medicinal Chemistry. 53: 6550-9. PMID 20806896 DOI: 10.1021/jm1008538 |
0.301 |
|
| 2010 |
Valant C, Aurelio L, Urmaliya VB, White P, Scammells PJ, Sexton PM, Christopoulos A. Delineating the mode of action of adenosine A1 receptor allosteric modulators. Molecular Pharmacology. 78: 444-55. PMID 20547736 DOI: 10.1124/mol.110.064568 |
0.384 |
|
| 2010 |
Devine SM, Gregg A, Figler H, McIntosh K, Urmaliya V, Linden J, Pouton CW, White PJ, Bottle SE, Scammells PJ. Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. Bioorganic & Medicinal Chemistry. 18: 3078-87. PMID 20385496 DOI: 10.1016/J.Bmc.2010.03.047 |
0.314 |
|
| 2010 |
HARDEN FA, QUINN RJ, SCAMMELLS PJ. ChemInform Abstract: Synthesis and Adenosine Receptor Affinity of a Series of Pyrazolo(3,4- d)pyrimidine Analogues of 1-Methylisoguanosine. Cheminform. 23: no-no. DOI: 10.1002/CHIN.199210201 |
0.363 |
|
| 2009 |
Aurelio L, Valant C, Figler H, Flynn BL, Linden J, Sexton PM, Christopoulos A, Scammells PJ. 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. Bioorganic & Medicinal Chemistry. 17: 7353-61. PMID 19751980 DOI: 10.1016/J.Bmc.2009.08.024 |
0.319 |
|
| 2009 |
Stewart GD, Valant C, Dowell SJ, Mijaljica D, Devenish RJ, Scammells PJ, Sexton PM, Christopoulos A. Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity. The Journal of Pharmacology and Experimental Therapeutics. 331: 277-86. PMID 19641164 DOI: 10.1124/jpet.109.158667 |
0.349 |
|
| 2008 |
Karellas P, McNaughton M, Baker SP, Scammells PJ. Synthesis of bivalent β2-adrenergic and adenosine A 1 receptor ligands Journal of Medicinal Chemistry. 51: 6128-6137. PMID 18783211 DOI: 10.1021/jm800613s |
0.329 |
|
| 2008 |
Ferguson GN, Valant C, Horne J, Figler H, Flynn BL, Linden J, Chalmers DK, Sexton PM, Christopoulos A, Scammells PJ. 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. Journal of Medicinal Chemistry. 51: 6165-72. PMID 18771255 DOI: 10.1021/Jm800557D |
0.413 |
|
| 2008 |
Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, Christopoulos A. A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. The Journal of Biological Chemistry. 283: 29312-21. PMID 18723515 DOI: 10.1074/jbc.M803801200 |
0.451 |
|
| 2007 |
Gregg A, Bottle SE, Devine SM, Figler H, Linden J, White P, Pouton CW, Urmaliya V, Scammells PJ. Dual acting antioxidant A1 adenosine receptor agonists. Bioorganic & Medicinal Chemistry Letters. 17: 5437-41. PMID 17689079 DOI: 10.1016/J.Bmcl.2007.07.035 |
0.314 |
|
| 2004 |
Hutchinson SA, Baker SP, Linden J, Scammells PJ. New potent and selective A1 adenosine receptor agonists. Bioorganic & Medicinal Chemistry. 12: 4877-84. PMID 15336267 DOI: 10.1016/j.bmc.2004.07.004 |
0.319 |
|
| 2004 |
Hutchinson SA, Scammells PJ. A(1) adenosine receptor agonists: medicinal chemistry and therapeutic potential. Current Pharmaceutical Design. 10: 2021-39. PMID 15279543 DOI: 10.2174/1381612043384204 |
0.326 |
|
| 2002 |
Hutchinson SA, Baker SP, Scammells PJ. New 2,N6-disubstituted adenosines: potent and selective A1 adenosine receptor agonists. Bioorganic & Medicinal Chemistry. 10: 1115-22. PMID 11836122 DOI: 10.1016/S0968-0896(01)00384-4 |
0.325 |
|
| 2001 |
Beauglehole AR, Baker SP, Scammells PJ. Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A(1)-adenosine receptor. Journal of Medicinal Chemistry. 43: 4973-80. PMID 11150167 DOI: 10.1021/JM000181F |
0.339 |
|
| 1999 |
Scammells PJ, Baker SP, Beauglehole AR. XH-14 analogues as adenosine antagonists. Bioorganic & Medicinal Chemistry. 6: 1517-24. PMID 9801823 DOI: 10.1016/S0968-0896(98)00093-5 |
0.374 |
|
| 1992 |
Harden F, Jordan L, McKirdy J, Quinn RJ, Scammells P, Willis RJ. Radioligand binding and cardiovascular effects of a new adenosine antagonist Journal of Molecular and Cellular Cardiology. 24. DOI: 10.1016/0022-2828(92)93131-3 |
0.355 |
|
| 1991 |
Harden FA, Quinn RJ, Scammells PJ. Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine. Journal of Medicinal Chemistry. 34: 2892-8. PMID 1895306 DOI: 10.1021/JM00113A031 |
0.373 |
|
| 1991 |
Quinn R, Scammells P, Tucker D. Mono-α-carbamoylethylthio-substituted pyrazolo[3,4-d]pyrimidines: The position of substitution Australian Journal of Chemistry. 44: 753-757. DOI: 10.1071/Ch9910753 |
0.446 |
|
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