Year |
Citation |
Score |
2023 |
Dekkers S, Comez D, Karsai N, Arimont-Segura M, Canals M, Caspar B, de Graaf C, Kilpatrick LE, Leurs R, Kellam B, Hill SJ, Briddon SJ, Stocks MJ. Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3). Acs Medicinal Chemistry Letters. 15: 143-148. PMID 38229752 DOI: 10.1021/acsmedchemlett.3c00469 |
0.568 |
|
2023 |
Dekkers S, Caspar B, Goulding J, Kindon ND, Kilpatrick LE, Stoddart LA, Briddon SJ, Kellam B, Hill SJ, Stocks MJ. Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor. Journal of Medicinal Chemistry. PMID 36944083 DOI: 10.1021/acs.jmedchem.3c00151 |
0.561 |
|
2022 |
Kok ZY, Stoddart LA, Mistry SJ, Mocking TAM, Vischer HF, Leurs R, Hill SJ, Mistry SN, Kellam B. Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H Receptor. Journal of Medicinal Chemistry. 65: 8258-8288. PMID 35734860 DOI: 10.1021/acs.jmedchem.2c00125 |
0.794 |
|
2021 |
Goulding J, Mistry SJ, Soave M, Woolard J, Briddon SJ, White CW, Kellam B, Hill SJ. Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2-adrenoceptor in CRISPR/Cas9 genome-edited HEK293T cells at low expression levels. Pharmacology Research & Perspectives. 9: e00779. PMID 34003582 DOI: 10.1002/prp2.779 |
0.519 |
|
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 |
0.697 |
|
2021 |
Stoddart LA, Kilpatrick LE, Corriden R, Kellam B, Briddon SJ, Hill SJ. Efficient G protein coupling is not required for agonist-mediated internalization and membrane reorganization of the adenosine A receptor. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 35: e21211. PMID 33710641 DOI: 10.1096/fj.202001729RR |
0.521 |
|
2020 |
Stoddart LA, Kindon ND, Otun O, Harwood CR, Patera F, Veprintsev DB, Woolard J, Briddon SJ, Franks HA, Hill SJ, Kellam B. Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells. Communications Biology. 3: 722. PMID 33247190 DOI: 10.1038/s42003-020-01451-w |
0.551 |
|
2020 |
Baker JG, Fromont C, Bruder M, Thompson KSJ, Kellam B, Hill SJ, Gardiner SM, Fischer PM. Using Esterase Selectivity to Determine the Duration of Systemic Availability and Abolish Systemic Side Effects of Topical β-Blockers. Acs Pharmacology & Translational Science. 3: 737-748. PMID 32832874 DOI: 10.1021/acsptsci.0c00051 |
0.39 |
|
2020 |
Soave M, Heukers R, Kellam B, Woolard J, Smit MJ, Briddon SJ, Hill SJ. Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies. Cell Chemical Biology. PMID 32610042 DOI: 10.1016/J.Chembiol.2020.06.006 |
0.566 |
|
2020 |
Gillis A, Gondin AB, Kliewer A, Sanchez J, Lim HD, Alamein C, Manandhar P, Santiago M, Fritzwanker S, Schmidel F, Katte TA, Reekie T, Grimsey NL, Kassiou M, Kellam B, et al. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Science Signaling. 13. PMID 32234959 DOI: 10.1126/Scisignal.Aaz3140 |
0.423 |
|
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 |
0.735 |
|
2019 |
Mistry SN, Marchand P, Kellam B. 27th Annual GP2A Medicinal Chemistry Conference. Pharmaceuticals (Basel, Switzerland). 12. PMID 31817636 DOI: 10.3390/Ph12040179 |
0.724 |
|
2019 |
Soave M, Kellam B, Woolard J, Briddon SJ, Hill SJ. NanoBiT Complementation to Monitor Agonist-Induced Adenosine A Receptor Internalization. Slas Discovery : Advancing Life Sciences R & D. 2472555219880475. PMID 31583945 DOI: 10.1177/2472555219880475 |
0.583 |
|
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 |
0.751 |
|
2019 |
Adlere I, Caspar B, Arimont M, Dekkers S, Visser K, Stuijt J, de Graaf C, Stocks M, Kellam B, Briddon S, Wijtmans M, de Esch I, Hill S, Leurs R. Modulators of CXCR4 and CXCR7/ACKR3 function. Molecular Pharmacology. PMID 31548340 DOI: 10.1124/Mol.119.117663 |
0.62 |
|
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 |
0.759 |
|
2018 |
Alcobia DC, Ziegler AI, Kondrashov A, Comeo E, Mistry S, Kellam B, Chang A, Woolard J, Hill SJ, Sloan EK. Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET. Iscience. 6: 280-288. PMID 30240618 DOI: 10.1016/J.Isci.2018.08.006 |
0.528 |
|
2018 |
Conroy S, Kindon ND, Glenn J, Stoddart LA, Lewis RJ, Hill SJ, Kellam B, Stocks MJ. Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y Receptor Based on AR-C118925. Journal of Medicinal Chemistry. PMID 29688707 DOI: 10.1021/Acs.Jmedchem.8B00606 |
0.576 |
|
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 |
0.767 |
|
2018 |
Conroy S, Kindon ND, Glenn J, Stoddart LA, Lewis RJ, Hill SJ, Kellam B, Stocks MJ. Synthesis and Evaluation of the first Fluorescent Antagonists of the Human P2YReceptor based on AR-C118925. Journal of Medicinal Chemistry. PMID 29558126 DOI: 10.1021/Acs.Jmedchem.8B00139 |
0.622 |
|
2018 |
Citossi F, Smith T, Lee JB, Segal J, Gershkovich P, Stocks MJ, Bradshaw TD, Kellam B, Marlow M. Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation. Molecular Pharmaceutics. PMID 29502421 DOI: 10.1021/Acs.Molpharmaceut.7B01106 |
0.319 |
|
2018 |
Stoddart LA, Vernall AJ, Bouzo-Lorenzo M, Bosma R, Kooistra AJ, de Graaf C, Vischer HF, Leurs R, Briddon SJ, Kellam B, Hill SJ. Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports. 8: 1572. PMID 29371669 DOI: 10.1038/S41598-018-19714-2 |
0.632 |
|
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 |
0.604 |
|
2017 |
Arruda MA, Stoddart LA, Gherbi K, Briddon SJ, Kellam B, Hill SJ. A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells. Frontiers in Pharmacology. 8: 908. PMID 29321740 DOI: 10.3389/Fphar.2017.00908 |
0.622 |
|
2017 |
Baker JG, Gardiner SM, Woolard J, Fromont C, Jadhav GP, Mistry SN, Thompson KS, Kellam B, Hill SJ, Fischer PM. Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. PMID 28400472 DOI: 10.1096/Fj.201601305R |
0.748 |
|
2017 |
Schwehm C, Kellam B, Garces AE, Hill PS, Kindon ND, Bradshaw TD, Li J, Macdonald SJ, Rowedder JE, Stoddart LA, Stocks MJ. Design and elaboration of a tractable tricyclic scaffold to synthesize drug-like inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C-C chemokine receptor type 5 (CCR5), and highly potent and selective phosphoinositol-3 kinase δ (PI3Kδ) inhibitors. Journal of Medicinal Chemistry. PMID 28128944 DOI: 10.1021/Acs.Jmedchem.6B01801 |
0.391 |
|
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 |
0.476 |
|
2016 |
Emtage AL, Mistry SN, Fischer PM, Kellam B, Laughton CA. GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors. Journal of Biomolecular Structure & Dynamics. 1-47. PMID 27532213 DOI: 10.1080/07391102.2016.1226197 |
0.783 |
|
2016 |
Conroy S, Kindon N, Kellam B, Stocks MJ. Drug-like Antagonists of P2Y Receptors-From Lead Identification to Drug Development. Journal of Medicinal Chemistry. 59: 9981-10005. PMID 27413802 DOI: 10.1021/Acs.Jmedchem.5B01972 |
0.443 |
|
2016 |
Disney AJ, Kellam B, Dekker LV. Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications. Chemmedchem. 11: 972-9. PMID 27008372 DOI: 10.1002/Cmdc.201500589 |
0.331 |
|
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 |
0.653 |
|
2015 |
Stoddart LA, Vernall AJ, Briddon SJ, Kellam B, Hill SJ. Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist. Neuropharmacology. 98: 68-77. PMID 25937210 DOI: 10.1016/J.Neuropharm.2015.04.013 |
0.604 |
|
2014 |
Schwehm C, Lewis W, Blake AJ, Kellam B, Stocks MJ. Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate. Acta Crystallographica. Section C, Structural Chemistry. 70: 1161-8. PMID 25471418 DOI: 10.1107/S205322961402436X |
0.309 |
|
2014 |
Corriden R, Kilpatrick LE, Kellam B, Briddon SJ, Hill SJ. Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 28: 4211-22. PMID 24970394 DOI: 10.1096/Fj.13-247270 |
0.6 |
|
2014 |
Stoddart LA, Kellam B, Briddon SJ, Hill SJ. Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization. British Journal of Pharmacology. 171: 3827-44. PMID 24750014 DOI: 10.1111/Bph.12739 |
0.562 |
|
2014 |
Hill SJ, May LT, Kellam B, Woolard J. Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization. British Journal of Pharmacology. 171: 1102-13. PMID 24024783 DOI: 10.1111/Bph.12345 |
0.595 |
|
2014 |
Vernall AJ, Hill SJ, Kellam B. The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs. British Journal of Pharmacology. 171: 1073-84. PMID 23734587 DOI: 10.1111/Bph.12265 |
0.573 |
|
2013 |
Dickens MP, Roxburgh P, Hock A, Mezna M, Kellam B, Vousden KH, Fischer PM. 5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2. Bioorganic & Medicinal Chemistry. 21: 6868-77. PMID 24113239 DOI: 10.1016/J.Bmc.2013.09.038 |
0.316 |
|
2013 |
Vernall AJ, Stoddart LA, Briddon SJ, Ng HW, Laughton CA, Doughty SW, Hill SJ, Kellam B. Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers. Organic & Biomolecular Chemistry. 11: 5673-82. PMID 23881285 DOI: 10.1039/C3Ob41221K |
0.657 |
|
2013 |
Corriden R, Self T, Akong-Moore K, Nizet V, Kellam B, Briddon SJ, Hill SJ. Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. Embo Reports. 14: 726-32. PMID 23817552 DOI: 10.1038/Embor.2013.89 |
0.548 |
|
2013 |
Mistry SN, Baker JG, Fischer PM, Hill SJ, Gardiner SM, Kellam B. Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists. Journal of Medicinal Chemistry. 56: 3852-65. PMID 23614528 DOI: 10.1021/Jm400348G |
0.78 |
|
2012 |
Stoddart LA, Vernall AJ, Denman JL, Briddon SJ, Kellam B, Hill SJ. Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Chemistry & Biology. 19: 1105-15. PMID 22999879 DOI: 10.1016/J.Chembiol.2012.07.014 |
0.637 |
|
2012 |
Vernall AJ, Stoddart LA, Briddon SJ, Hill SJ, Kellam B. Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold. Journal of Medicinal Chemistry. 55: 1771-82. PMID 22277057 DOI: 10.1021/Jm201722Y |
0.637 |
|
2012 |
Dale CL, Hill SJ, Kellam B. New potent, short-linker BODIPY-630/650™ labelled fluorescent adenosine receptor agonists Medchemcomm. 3: 333-338. DOI: 10.1039/C2Md00247G |
0.63 |
|
2011 |
Baker JG, Adams LA, Salchow K, Mistry SN, Middleton RJ, Hill SJ, Kellam B. Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. Journal of Medicinal Chemistry. 54: 6874-87. PMID 21870877 DOI: 10.1021/Jm2008562 |
0.801 |
|
2011 |
Briddon SJ, Kellam B, Hill SJ. Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells. Methods in Molecular Biology (Clifton, N.J.). 746: 211-36. PMID 21607859 DOI: 10.1007/978-1-61779-126-0_11 |
0.611 |
|
2010 |
Baker JG, Middleton R, Adams L, May LT, Briddon SJ, Kellam B, Hill SJ. Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands. British Journal of Pharmacology. 159: 772-86. PMID 20105183 DOI: 10.1111/J.1476-5381.2009.00488.X |
0.635 |
|
2008 |
Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ. Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 22: 850-60. PMID 17959910 DOI: 10.1096/Fj.07-8180Com |
0.568 |
|
2007 |
Middleton RJ, Briddon SJ, Cordeaux Y, Yates AS, Dale CL, George MW, Baker JG, Hill SJ, Kellam B. New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells. Journal of Medicinal Chemistry. 50: 782-93. PMID 17249651 DOI: 10.1021/Jm061279I |
0.628 |
|
2005 |
AbuKhader M, Heap J, De Matteis C, Kellam B, Doughty SW, Minton N, Paoli M. Binding of the anticancer prodrug CB1954 to the activating enzyme NQO2 revealed by the crystal structure of their complex. Journal of Medicinal Chemistry. 48: 7714-9. PMID 16302811 DOI: 10.1021/Jm050730N |
0.303 |
|
2005 |
Middleton RJ, Kellam B. Fluorophore-tagged GPCR ligands. Current Opinion in Chemical Biology. 9: 517-25. PMID 16125436 DOI: 10.1016/J.Cbpa.2005.08.016 |
0.472 |
|
2005 |
Yates AS, Doughty SW, Kendall DA, Kellam B. Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor. Bioorganic & Medicinal Chemistry Letters. 15: 3758-62. PMID 15993070 DOI: 10.1016/J.Bmcl.2005.05.049 |
0.488 |
|
2004 |
Briddon SJ, Middleton RJ, Cordeaux Y, Flavin FM, Weinstein JA, George MW, Kellam B, Hill SJ. Quantitative analysis of the formation and diffusion of A1-adenosine receptor-antagonist complexes in single living cells. Proceedings of the National Academy of Sciences of the United States of America. 101: 4673-8. PMID 15070776 DOI: 10.1073/Pnas.0400420101 |
0.573 |
|
2004 |
Briddon SJ, Middleton RJ, Yates AS, George MW, Kellam B, Hill SJ. Application of fluorescence correlation spectroscopy to the measurement of agonist binding to a G-protein coupled receptor at the single cell level. Faraday Discussions. 126: 197-207; discussion . PMID 14992407 DOI: 10.1039/B307407B |
0.561 |
|
1998 |
Kellam B, Drouillat B, Dekany G, Starr MS, Toth I. Synthesis and in vitro evaluation of lipoamino acid and carbohydrate-modified enkephalins as potential antinociceptive agents International Journal of Pharmaceutics. 161: 55-64. DOI: 10.1016/S0378-5173(97)00328-1 |
0.367 |
|
1997 |
Drouillat B, Kellam B, Dekany G, Starr MS, Toth I. Solid phase synthesis of C-terminal carbohydrate modified enkephalins Bioorganic and Medicinal Chemistry Letters. 7: 2247-2250. DOI: 10.1016/S0960-894X(97)00395-8 |
0.399 |
|
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