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For: Young RJ, Leeson PD. Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations. J Med Chem 2018;61:6421-67. [DOI: 10.1021/acs.jmedchem.8b00180] [Cited by in Crossref: 40] [Cited by in F6Publishing: 34] [Article Influence: 10.0] [Reference Citation Analysis]
Number Citing Articles
1 Shultz MD. Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs: Miniperspective. J Med Chem 2019;62:1701-14. [DOI: 10.1021/acs.jmedchem.8b00686] [Cited by in Crossref: 132] [Cited by in F6Publishing: 112] [Article Influence: 33.0] [Reference Citation Analysis]
2 Borthwick JA, Alemparte C, Wall I, Whitehurst BC, Argyrou A, Burley G, de Dios-Anton P, Guijarro L, Monteiro MC, Ortega F, Suckling CJ, Pichel JC, Cacho M, Young RJ. Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity. J Med Chem 2020;63:2557-76. [PMID: 31922409 DOI: 10.1021/acs.jmedchem.9b01561] [Cited by in Crossref: 5] [Cited by in F6Publishing: 2] [Article Influence: 2.5] [Reference Citation Analysis]
3 Bunally SB, Luscombe CN, Young RJ. Using Physicochemical Measurements to Influence Better Compound Design. SLAS Discov 2019;24:791-801. [PMID: 31429385 DOI: 10.1177/2472555219859845] [Cited by in Crossref: 5] [Cited by in F6Publishing: 4] [Article Influence: 1.7] [Reference Citation Analysis]
4 Manevski N, King L, Pitt WR, Lecomte F, Toselli F. Metabolism by Aldehyde Oxidase: Drug Design and Complementary Approaches to Challenges in Drug Discovery. J Med Chem 2019;62:10955-94. [PMID: 31385704 DOI: 10.1021/acs.jmedchem.9b00875] [Cited by in Crossref: 30] [Cited by in F6Publishing: 25] [Article Influence: 10.0] [Reference Citation Analysis]
5 Jeffries B, Wang Z, Felstead HR, Le Questel J, Scott JS, Chiarparin E, Graton J, Linclau B. Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs. J Med Chem 2020;63:1002-31. [DOI: 10.1021/acs.jmedchem.9b01172] [Cited by in Crossref: 29] [Cited by in F6Publishing: 21] [Article Influence: 14.5] [Reference Citation Analysis]
6 Wuelfing WP, El Marrouni A, Lipert MP, Daublain P, Kesisoglou F, Converso A, Templeton AC. Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery. J Med Chem . [DOI: 10.1021/acs.jmedchem.1c01687] [Reference Citation Analysis]
7 Békés M, Langley DR, Crews CM. PROTAC targeted protein degraders: the past is prologue. Nat Rev Drug Discov 2022. [PMID: 35042991 DOI: 10.1038/s41573-021-00371-6] [Reference Citation Analysis]
8 Bhanot A, Sundriyal S. Physicochemical Profiling and Comparison of Research Antiplasmodials and Advanced Stage Antimalarials with Oral Drugs. ACS Omega 2021;6:6424-37. [PMID: 33718733 DOI: 10.1021/acsomega.1c00104] [Reference Citation Analysis]
9 Tinworth CP, Young RJ. Facts, Patterns, and Principles in Drug Discovery: Appraising the Rule of 5 with Measured Physicochemical Data. J Med Chem 2020;63:10091-108. [PMID: 32324397 DOI: 10.1021/acs.jmedchem.9b01596] [Cited by in Crossref: 15] [Cited by in F6Publishing: 11] [Article Influence: 7.5] [Reference Citation Analysis]
10 Goldberg FW, Finlay MRV, Ting AKT, Beattie D, Lamont GM, Fallan C, Wrigley GL, Schimpl M, Howard MR, Williamson B, Vazquez-Chantada M, Barratt DG, Davies BR, Cadogan EB, Ramos-Montoya A, Dean E. The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor. J Med Chem 2020;63:3461-71. [PMID: 31851518 DOI: 10.1021/acs.jmedchem.9b01684] [Cited by in Crossref: 11] [Cited by in F6Publishing: 10] [Article Influence: 5.5] [Reference Citation Analysis]
11 Villemure E, Terrett JA, Larouche-Gauthier R, Déry M, Chen H, Reese RM, Shields SD, Chen J, Magnuson S, Volgraf M. A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists. ACS Med Chem Lett 2021;12:1230-7. [PMID: 34413952 DOI: 10.1021/acsmedchemlett.1c00305] [Cited by in Crossref: 2] [Cited by in F6Publishing: 2] [Article Influence: 2.0] [Reference Citation Analysis]
12 Reiher CA, Schuman DP, Simmons N, Wolkenberg SE. Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens. ACS Med Chem Lett 2021;12:343-50. [PMID: 33738060 DOI: 10.1021/acsmedchemlett.0c00615] [Cited by in Crossref: 9] [Cited by in F6Publishing: 9] [Article Influence: 9.0] [Reference Citation Analysis]
13 Al-Khawaldeh I, Al Yasiri MJ, Aldred GG, Basmadjian C, Bordoni C, Harnor SJ, Heptinstall AB, Hobson SJ, Jennings CE, Khalifa S, Lebraud H, Martin MP, Miller DC, Shrives HJ, de Souza JV, Stewart HL, Temple M, Thomas HD, Totobenazara J, Tucker JA, Tudhope SJ, Wang LZ, Bronowska AK, Cano C, Endicott JA, Golding BT, Hardcastle IR, Hickson I, Wedge SR, Willmore E, Noble MEM, Waring MJ. An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase. J Med Chem 2021;64:10001-18. [PMID: 34212719 DOI: 10.1021/acs.jmedchem.0c01249] [Reference Citation Analysis]
14 Babbar P, Das P, Manickam Y, Mankad Y, Yadav S, Parvez S, Sharma A, Reddy DS. Design, Synthesis, and Structural Analysis of Cladosporin-Based Inhibitors of Malaria Parasites. ACS Infect Dis 2021;7:1777-94. [PMID: 33843204 DOI: 10.1021/acsinfecdis.1c00092] [Cited by in Crossref: 2] [Cited by in F6Publishing: 2] [Article Influence: 2.0] [Reference Citation Analysis]
15 Szabó G, Erdélyi P, Kolok S, Vastag M, Halász AS, Kis-Varga I, Lévay GI, Béni Z, Kóti J, Greiner I, Keserű GM. Fragment-Based Optimization of Dihydropyrazino-Benzimidazolones as Metabotropic Glutamate Receptor-2 Positive Allosteric Modulators against Migraine. J Med Chem 2021;64:8607-20. [PMID: 34080424 DOI: 10.1021/acs.jmedchem.1c00563] [Reference Citation Analysis]
16 Fullam E, Young RJ. Physicochemical properties and Mycobacterium tuberculosis transporters: keys to efficacious antitubercular drugs? RSC Med Chem 2020;12:43-56. [PMID: 34041481 DOI: 10.1039/d0md00265h] [Cited by in Crossref: 5] [Cited by in F6Publishing: 3] [Article Influence: 2.5] [Reference Citation Analysis]
17 McGonagle K, Tarver GJ, Cantizani J, Cotillo I, Dodd PG, Ferguson L, Gilbert IH, Marco M, Miles T, Naylor C, Osuna-Cabello M, Paterson C, Read KD, Pinto EG, Riley J, Scullion P, Shishikura Y, Simeons F, Stojanovski L, Svensen N, Thomas J, Wyatt PG, Manzano P, De Rycker M, Thomas MG. Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease. Eur J Med Chem 2022;238:114421. [PMID: 35594652 DOI: 10.1016/j.ejmech.2022.114421] [Reference Citation Analysis]
18 Kenny PW. The nature of ligand efficiency. J Cheminform 2019;11:8. [PMID: 30706294 DOI: 10.1186/s13321-019-0330-2] [Cited by in Crossref: 21] [Cited by in F6Publishing: 14] [Article Influence: 7.0] [Reference Citation Analysis]
19 Leeson PD, Bento AP, Gaulton A, Hersey A, Manners EJ, Radoux CJ, Leach AR. Target-Based Evaluation of "Drug-Like" Properties and Ligand Efficiencies. J Med Chem 2021;64:7210-30. [PMID: 33983732 DOI: 10.1021/acs.jmedchem.1c00416] [Cited by in F6Publishing: 1] [Reference Citation Analysis]
20 Depypere H, Lademacher C, Siddiqui E, Fraser GL. Fezolinetant in the treatment of vasomotor symptoms associated with menopause. Expert Opin Investig Drugs 2021;30:681-94. [PMID: 33724119 DOI: 10.1080/13543784.2021.1893305] [Reference Citation Analysis]
21 Ermondi G, Vallaro M, Goetz G, Shalaeva M, Caron G. Updating the portfolio of physicochemical descriptors related to permeability in the beyond the rule of 5 chemical space. Eur J Pharm Sci 2020;146:105274. [PMID: 32088315 DOI: 10.1016/j.ejps.2020.105274] [Cited by in Crossref: 9] [Cited by in F6Publishing: 8] [Article Influence: 4.5] [Reference Citation Analysis]
22 Holenz J, Stoy P. Advances in Lead Generation. Bioorganic & Medicinal Chemistry Letters 2019;29:517-24. [DOI: 10.1016/j.bmcl.2018.12.001] [Cited by in Crossref: 18] [Cited by in F6Publishing: 13] [Article Influence: 6.0] [Reference Citation Analysis]
23 Cruz CD, Wrigstedt P, Moslova K, Iashin V, Mäkkylä H, Ghemtio L, Heikkinen S, Tammela P, Perea-Buceta JE. Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation. Eur J Med Chem 2021;211:113002. [PMID: 33223262 DOI: 10.1016/j.ejmech.2020.113002] [Cited by in Crossref: 1] [Article Influence: 0.5] [Reference Citation Analysis]
24 Giustiniano M, Gruber CW, Kent CN, Trippier PC. Back to the Medicinal Chemistry Future. J Med Chem 2021;64:15515-8. [PMID: 34719927 DOI: 10.1021/acs.jmedchem.1c01788] [Reference Citation Analysis]
25 Pennington LD, Aquila BM, Choi Y, Valiulin RA, Muegge I. Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design. J Med Chem 2020;63:8956-76. [PMID: 32330036 DOI: 10.1021/acs.jmedchem.9b02092] [Cited by in Crossref: 9] [Cited by in F6Publishing: 7] [Article Influence: 4.5] [Reference Citation Analysis]
26 Brown DG, Wobst HJ. A Decade of FDA-Approved Drugs (2010-2019): Trends and Future Directions. J Med Chem 2021;64:2312-38. [PMID: 33617254 DOI: 10.1021/acs.jmedchem.0c01516] [Cited by in Crossref: 8] [Cited by in F6Publishing: 9] [Article Influence: 8.0] [Reference Citation Analysis]
27 Forte B, Ottilie S, Plater A, Campo B, Dechering KJ, Gamo FJ, Goldberg DE, Istvan ES, Lee M, Lukens AK, McNamara CW, Niles JC, Okombo J, Pasaje CFA, Siegel MG, Wirth D, Wyllie S, Fidock DA, Baragaña B, Winzeler EA, Gilbert IH. Prioritization of Molecular Targets for Antimalarial Drug Discovery. ACS Infect Dis 2021;7:2764-76. [PMID: 34523908 DOI: 10.1021/acsinfecdis.1c00322] [Reference Citation Analysis]
28 Troup RI, Jeffries B, Saudain RE, Georgiou E, Fish J, Scott JS, Chiarparin E, Fallan C, Linclau B. Skipped Fluorination Motifs: Synthesis of Building Blocks and Comparison of Lipophilicity Trends with Vicinal and Isolated Fluorination Motifs. J Org Chem 2021;86:1882-900. [DOI: 10.1021/acs.joc.0c02810] [Cited by in Crossref: 1] [Cited by in F6Publishing: 1] [Article Influence: 1.0] [Reference Citation Analysis]
29 Brown DG, Boström J. Where Do Recent Small Molecule Clinical Development Candidates Come From? J Med Chem 2018;61:9442-68. [DOI: 10.1021/acs.jmedchem.8b00675] [Cited by in Crossref: 54] [Cited by in F6Publishing: 43] [Article Influence: 13.5] [Reference Citation Analysis]
30 Sosa Y, Deniskin R, Frame IJ, Steiginga MS, Bandyopadhyay D, Graybill TL, Kallal LA, Ouellette MT, Pope AJ, Widdowson KL, Young RJ, Akabas MH. Identification via a Parallel Hit Progression Strategy of Improved Small Molecule Inhibitors of the Malaria Purine Uptake Transporter that Inhibit Plasmodium falciparum Parasite Proliferation. ACS Infect Dis 2019;5:1738-53. [PMID: 31373203 DOI: 10.1021/acsinfecdis.9b00168] [Cited by in Crossref: 4] [Cited by in F6Publishing: 3] [Article Influence: 1.3] [Reference Citation Analysis]
31 Freidel MR, Armen RS. Mapping major SARS-CoV-2 drug targets and assessment of druggability using computational fragment screening: Identification of an allosteric small-molecule binding site on the Nsp13 helicase. PLoS One 2021;16:e0246181. [PMID: 33596235 DOI: 10.1371/journal.pone.0246181] [Cited by in Crossref: 2] [Article Influence: 2.0] [Reference Citation Analysis]
32 Wu G, Zhao T, Kang D, Zhang J, Song Y, Namasivayam V, Kongsted J, Pannecouque C, De Clercq E, Poongavanam V, Liu X, Zhan P. Overview of Recent Strategic Advances in Medicinal Chemistry. J Med Chem 2019;62:9375-414. [PMID: 31050421 DOI: 10.1021/acs.jmedchem.9b00359] [Cited by in Crossref: 44] [Cited by in F6Publishing: 36] [Article Influence: 14.7] [Reference Citation Analysis]
33 Subbaiah MAM, Meanwell NA. Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design. J Med Chem 2021;64:14046-128. [PMID: 34591488 DOI: 10.1021/acs.jmedchem.1c01215] [Reference Citation Analysis]
34 Pennington LD, Muegge I. Holistic drug design for multiparameter optimization in modern small molecule drug discovery. Bioorganic & Medicinal Chemistry Letters 2021;41:128003. [DOI: 10.1016/j.bmcl.2021.128003] [Cited by in Crossref: 3] [Cited by in F6Publishing: 2] [Article Influence: 3.0] [Reference Citation Analysis]
35 Debrauwer V, Leito I, Lõkov M, Tshepelevitsh S, Parmentier M, Blanchard N, Bizet V. Synthesis and Physicochemical Properties of 2-SF 5 -(Aza)Indoles, a New Family of SF 5 Heterocycles. ACS Org Inorg Au 2021;1:43-50. [DOI: 10.1021/acsorginorgau.1c00010] [Cited by in Crossref: 8] [Cited by in F6Publishing: 4] [Article Influence: 8.0] [Reference Citation Analysis]
36 De Rycker M, Horn D, Aldridge B, Amewu RK, Barry CE 3rd, Buckner FS, Cook S, Ferguson MAJ, Gobeau N, Herrmann J, Herrling P, Hope W, Keiser J, Lafuente-Monasterio MJ, Leeson PD, Leroy D, Manjunatha UH, McCarthy J, Miles TJ, Mizrahi V, Moshynets O, Niles J, Overington JP, Pottage J, Rao SPS, Read KD, Ribeiro I, Silver LL, Southern J, Spangenberg T, Sundar S, Taylor C, Van Voorhis W, White NJ, Wyllie S, Wyatt PG, Gilbert IH. Setting Our Sights on Infectious Diseases. ACS Infect Dis 2020;6:3-13. [PMID: 31808676 DOI: 10.1021/acsinfecdis.9b00371] [Cited by in Crossref: 9] [Cited by in F6Publishing: 9] [Article Influence: 4.5] [Reference Citation Analysis]
37 Boström J, Brown DG, Young RJ, Keserü GM. Expanding the medicinal chemistry synthetic toolbox. Nat Rev Drug Discov 2018;17:709-27. [DOI: 10.1038/nrd.2018.116] [Cited by in Crossref: 175] [Cited by in F6Publishing: 140] [Article Influence: 43.8] [Reference Citation Analysis]
38 Linclau B, Wang Z, Jeffries B, Graton J, Carbajo RJ, Sinnaeve D, Le Questel JY, Scott JS, Chiarparin E. Relating Conformational Equilibria to Conformer-Specific Lipophilicities: New Opportunities in Drug Discovery. Angew Chem Int Ed Engl 2021;:e202114862. [PMID: 34913249 DOI: 10.1002/anie.202114862] [Reference Citation Analysis]
39 Davis OA, Cheung KJ, Brennan A, Lloyd MG, Rodrigues MJ, Pierrat OA, Collie GW, Le Bihan YV, Huckvale R, Harnden AC, Varela A, Bright MD, Eve P, Hayes A, Henley AT, Carter MD, McAndrew PC, Talbot R, Burke R, van Montfort RLM, Raynaud FI, Rossanese OW, Meniconi M, Bellenie BR, Hoelder S. Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors. J Med Chem 2022. [PMID: 35657291 DOI: 10.1021/acs.jmedchem.1c02174] [Reference Citation Analysis]
40 Kuzmina OM, Weisel M, Narine AA. 5‐Membered Mesoionic Insecticides: Synthesis and Evaluation of 1,3,4‐Thiadiazol‐4‐ium‐2‐olates with High Affinity for the Insect Nicotinic Acetylcholine Receptor. Eur J Org Chem 2019;2019:5527-31. [DOI: 10.1002/ejoc.201900637] [Cited by in Crossref: 4] [Cited by in F6Publishing: 2] [Article Influence: 1.3] [Reference Citation Analysis]
41 Bryan MC, Drobnick J, Gobbi A, Kolesnikov A, Chen Y, Rajapaksa N, Ndubaku C, Feng J, Chang W, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Huang Z, Sujatha-Bhaskar S, Brightbill H, DiPasquale A, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR. Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors. J Med Chem 2019;62:6223-40. [PMID: 31082230 DOI: 10.1021/acs.jmedchem.9b00439] [Cited by in Crossref: 12] [Cited by in F6Publishing: 10] [Article Influence: 4.0] [Reference Citation Analysis]
42 Helal CJ, Bundesmann M, Hammond S, Holmstrom M, Klug-McLeod J, Lefker BA, McLeod D, Subramanyam C, Zakaryants O, Sakata S. Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis. ACS Med Chem Lett 2019;10:1104-9. [PMID: 31413793 DOI: 10.1021/acsmedchemlett.9b00205] [Cited by in Crossref: 16] [Cited by in F6Publishing: 14] [Article Influence: 5.3] [Reference Citation Analysis]
43 Linclau B, Wang Z, Jeffries B, Graton J, Carbajo RJ, Sinnaeve D, Le Questel J, Scott JS, Chiarparin E. Relating Conformational Equilibria to Conformer‐Specific Lipophilicities: New Opportunities in Drug Discovery. Angewandte Chemie. [DOI: 10.1002/ange.202114862] [Reference Citation Analysis]
44 Veale CGL. Into the Fray! A Beginner's Guide to Medicinal Chemistry. ChemMedChem 2021;16:1199-225. [PMID: 33591595 DOI: 10.1002/cmdc.202000929] [Reference Citation Analysis]