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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings 1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997) 3–25. 1

Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139

Goodman & Gilman's The Pharmacological Basis of Therapeutics

Brunton, L. L. (1985) · Cited by 7,321

DrugBank: a comprehensive resource for in silico drug discovery and exploration

Wishart, D. S. (2006) · Nucleic Acids Research · doi:10.1093/nar/gkj067 · Cited by 3,892

How to improve R&D productivity: the pharmaceutical industry's grand challenge

Paul, S. M., Mytelka, D. S., Dunwiddie, C. T., Persinger, C. C., Munos, B. H., Lindborg, S. R., & Schacht, A. L. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3078 · Cited by 3,566

How many drug targets are there?

Overington, J. P., Al-Lazikani, B., & Hopkins, A. L. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2199 · Cited by 3,505

The druggable genome

Hopkins, A. L., & Groom, C. R. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd892 · Cited by 3,305

Targeting cancer with small molecule kinase inhibitors

Zhang, J., Yang, P. L., & Gray, N. S. (2008) · Nature reviews. Cancer · doi:10.1038/nrc2559 · Cited by 2,648

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Cohen, P. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd773 · Cited by 2,232

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Knox, C., Law, V., Jewison, T., Liu, P., Ly, S., Frolkis, A., Pon, A., Banco, K., Mak, C., Neveu, V., et al. (2010) · Nucleic Acids Research · doi:10.1093/nar/gkq1126 · Cited by 1,832

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Larsen, C. M., Faulenbach, M., Vaag, A., Vølund, A., Ehses, J. A., Seifert, B., Mandrup-Poulsen, T., & Donath, M. Y. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa065213 · Cited by 1,798

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Rajkumar, P., & Pluznick, J. L. (2016) · Acta Physiologica · doi:10.1111/apha.12813 · Cited by 9

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Bhullar, K. S., Fan, H., Nael, M. A., Elokely, K. M., & Wu, J. (2023) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.3c01544 · Cited by 7

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Cappi, C., Oliphant, M. E., Péter, Z., Zai, G. C., Sullivan, C. A. W., Gupta, A. R., Hoffman, E. J., Virdee, M., Willsey, A. J., Shavitt, R. G., et al. (2017) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/127712 · Cited by 7

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Doyle, J. R., Harwood, B. N., Krishnaji, S. T., Krishnamurthy, V. M., Lin, W.-E., Fortin, J., Kumar, K., & Kopin, A. S. (2014) · PLoS ONE · doi:10.1371/journal.pone.0110502 · Cited by 6

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Pereira, P. H. S., Borges‐Pereira, L., & Garcia, C. R. S. (2020) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026620666200826122716 · Cited by 6

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Bibbe, J. M., & Vriend, G. (2021) · Proteins Structure Function and Bioinformatics · doi:10.1002/prot.26179 · Cited by 6

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Liebscher, I., Monk, K. R., & Schöneberg, T. (2015) · Oncotarget · doi:10.18632/oncotarget.5112 · Cited by 6

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Lankipalli, S., & Ramagopal, U. A. (2021) · Pharmacological Research · doi:10.1016/j.phrs.2021.105735 · Cited by 6

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Vass, M., Kooistra, A. J., Verhoeven, S., Gloriam, D. E. I., de Esch, I. J. P., & de Graaf, C. (2017) · Methods in molecular biology · doi:10.1007/978-1-4939-7465-8_4 · Cited by 5

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Kouassi, K. A. R., Ganiyou, A., Diomandé, D., Benié, A., & Ziao, N. (2022) · Computational Chemistry · doi:10.4236/cc.2022.102002 · Cited by 5

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Jiang, G., Sohn, S., Zimmermann, M. T., Wang, C., Liu, H., & Chute, C. G. (2015) · Europe PMC (PubMed Central) · Cited by 5

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Zamanzadeh, V., Ahmadi, F., Behshid, M., Irajpour, A., & Zakeri‐Milani, P. (2017) · Drug Research · doi:10.1055/s-0042-121420 · Cited by 5

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Struck, A. J., Walsh, B., Buchanan, A., Lee, J., Spangler, R. K., Stuart, J. M., & Ellrott, K. (2020) · JCO Clinical Cancer Informatics · doi:10.1200/cci.19.00110 · Cited by 5

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Ramdani, E. D., Yanuar, A., & Tjandrawinata, R. R. (2019) · Journal of Applied Pharmaceutical Science · doi:10.7324/japs.2019.90903 · Cited by 5

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Moya‐García, A. A., Adeyelu, T. T., Krüger, F. A., Dawson, N. L., Lees, J. G., Overington, J. P., Orengo, C. A., & Ranea, J. A. G. (2016) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/044289 · Cited by 5

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Singh, S. K., Agrawal, M., Pattanayak, A., Baidya, M., & Kumari, P. (2026) · Communications Biology · doi:10.1038/s42003-026-09516-y · Cited by 6

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Mori, Y., Tsuchihira, A., Yoshida, T., Yoshida, S., Fujiuchi, A., Ohmi, M., Isogai, Y., Sakaguchi, T., Eguchi, S., Tsuda, T., et al. (2021) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2021.112566 · Cited by 4

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Liu, Z., Li, H., Jin, Z., Li, Y., Guo, F., He, Y., Liu, X., Qi, Y., Yuan, L., He, F., et al. (2022) · Genomics Proteomics & Bioinformatics · doi:10.1016/j.gpb.2021.10.007 · Cited by 4

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Wang, D. H., & Park, J. Y. (2016) · Archives of Pathology & Laboratory Medicine · doi:10.5858/arpa.2015-0317-ra · Cited by 4

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Pinto, P. I. S., Miglioli, A., LaLone, C. A., Baumann, L., Baynes, A., Blanc, M., Cancio, I., Cousin, X., Dang, Z., Dumollard, R., et al. (2025) · Biological reviews/Biological reviews of the Cambridge Philosophical Society · doi:10.1111/brv.70106 · Cited by 3

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Qiu, C., Chen, J., Huang, H., Lin, Z., Zhang, Y., Liao, C., Yang, M., Qu, Y., Huang, S., Li, W., et al. (2022) · Gland Surgery · doi:10.21037/gs-22-453 · Cited by 2

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Krols, S., Matteucci, F., Hecke, K. V., Caljon, G., Jacobson, K. A., & Calenbergh, S. V. (2023) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.3c00427 · Cited by 3

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Sonawani, A., Naglekar, A., Kharche, S., & Sengupta, D. (2024) · Methods in molecular biology · doi:10.1007/978-1-0716-3985-6_13 · Cited by 3

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da Silva, S. P., da Costa, C. B. L., da Silva, J. D. F., Alves, R. R. D. V., Silva, G. A. D. S., de Freitas, A. F. S., Guedes, C. C. D. S., Marinho, A. D. O., Paiva, P. M. G., & Napoleão, T. H. (2021) · Research Society and Development · doi:10.33448/rsd-v10i2.12819 · Cited by 3

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Wang, J., Guo, C., Wei, X., Pu, X., Zhao, Y., Xu, C., & Wang, W. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26062822 · Cited by 2

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Schraink, T., Blumenberg, L. M., Hussey, G. A., George, S., Miller, B., Mathew, N., González-Robles, T. J., Sviderskiy, V. O., Papagiannakopoulos, T. Y., Possemato, R., et al. (2023) · Molecular & Cellular Proteomics · doi:10.1016/j.mcpro.2023.100596 · Cited by 3

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Wang, C., Bryliński, M., & Kurgan, L. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-816125-8.00028-6 · Cited by 2

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Chan, W. S., Zou, J., Ortiz, C. L. D., Chien, C.-H. C., Pan, R., & Yang, L. (2019) · Bioinformatics · doi:10.1093/bioinformatics/btz579 · Cited by 2

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Viereck, M., Gaulton, A., & Digles, D. (2017) · Methods and principles in medicinal chemistry · doi:10.1002/9783527679430.ch1 · Cited by 2

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Podder, A., & Latha, N. (2017) · Data in Brief · doi:10.1016/j.dib.2017.04.001 · Cited by 2

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Heydenreich, F. M., Plouffe, B., Rizk, A., Milić, D., Zhou, J., Breton, B., Gouill, C. L., Inoue, A., Bouvier, M., & Veprintsev, D. B. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.01.28.427950 · Cited by 2

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Vardanyan, V. H., Haldane, A., Hwang, H., Coskun, D., Lihan, M., Miller, E. B., Friesner, R. A., & Levy, R. M. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00312 · Cited by 1

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Miller, S. M., Moos, W. H., Munk, B. H., & Munk, S. A. (2016) · Elsevier eBooks · doi:10.1016/b978-0-08-100625-2.00011-8 · Cited by 1

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Hudson, I., Leemaqz, S., Shafi, S., & Abell, A. D. (2017) · MODSIM · doi:10.36334/modsim.2017.c6.hudson · Cited by 1

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González, Y., Guzmán‐Beltrán, S., Carreto-Binaghi, L. E., & Juárez, E. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-819811-7.00004-7 · Cited by 1

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Biroš, E., Birosova, E., & Moran, C. S. (2023) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2023.01.006 · Cited by 1

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Zhang, H., Ihara, M., & Chen, J. (2025) · Environmental Science & Technology · doi:10.1021/acs.est.5c05367 · Cited by 1

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Sigauke, L. T., Bishop, Ö. T., & Lobb, K. A. (2021) · Journal of Computational Biophysics and Chemistry · doi:10.1142/s2737416521500101 · Cited by 1

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Roth, B. L., Gotoh, Y., Giguère, P. M., & Nichols, D. E. (2018) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/251769 · Cited by 1

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Bernadyn, T. F., Kwarcinski, F. E., Chandan, N. R., Gandhi, R., Feng, Y., Holinstat, M. A., Parent, C. A., Smrcka, A. V., & Tall, G. G. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.09.11.675646 · Cited by 1

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Wang, R.-S., & Loscalzo, J. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-409547-2.12334-0

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Miller, S. M., Moos, W. H., Munk, B. H., & Munk, S. A. (2016) · Elsevier eBooks · doi:10.1016/b978-0-08-100625-2.00001-5

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Tomonaga, T. (2017) · Folia Pharmacologica Japonica · doi:10.1254/fpj.149.123

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Hingorani, A. D., Kuan, V., Finan, C., Krüger, F. A., Gaulton, A., Chopade, S., Sofat, R., MacAllister, R. J., Overington, J. P., Hemingway, H., et al. (2017) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/170142

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Pugsley, M. K., Abernathy, M. M., Whitney, T. M., Authier, S., Renger, J. J., & Curtis, M. J. (2018) · Elsevier eBooks · doi:10.1016/b978-0-12-812206-8.00015-7

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Seneci, P. (2018) · Elsevier eBooks · doi:10.1016/b978-0-08-099420-8.00001-8

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Espejo, M. S. (2019) · doi:10.35537/10915/73035

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Hong, S. Y. (2016)

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Attwood, M. M., & Schiöth, H. B. (2020) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2019.00386

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Hudson, I. L., Leemaqz, S., & Abell, A. D. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160233-00251

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Lansu, K. (2020) · Carolina Digital Repository (University of North Carolina at Chapel Hill) · doi:10.17615/p9r4-re19

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Agwuegbo, U., & Jonas, K. (2022) · Methods in cell biology · doi:10.1016/bs.mcb.2021.12.001

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袁, 鑫. (2022) · Advances in Clinical Medicine · doi:10.12677/acm.2022.123257

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Willardson, B. M., & Tensmeyer, N. C. (2017) · Wiley eBooks · doi:10.1002/9780470015902.a0027195

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Wang, X., van Westen, G. J. P., IJzerman, A. P., & Heitman, L. H. (2022) · Wiley eBooks · doi:10.1002/9781119564782.ch18

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Miller, S. M., Moos, W. H., Munk, B. H., Munk, S. A., Hart, C. P., & Spellmeyer, D. C. (2023) · Elsevier eBooks · doi:10.1016/b978-0-12-824304-6.00001-8

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LiangyongXia, Wu, Y. X., Zhao, L., Chen, L., Zhang, S., Wang, M., & Luo, J. (2023) · Research Square · doi:10.21203/rs.3.rs-3242419/v1

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Zegarra, L. A. D. (2023) · doi:10.35537/10915/156967

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Sun, Y. (2023) · Highlights in Science Engineering and Technology · doi:10.54097/hset.v66i.11708

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Bakulina, O., Sapegin, A., & Yarovaya, О. I. (2023) · Журнал органической химии · doi:10.31857/s0514749223120029

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Wang, R. S., Xu, H., & Loscalzo, J. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-29808-0.00025-x

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Otero-Carrasco, B., Santamaría, L. P., & Rodríguez‐González, A. (2025) · Proceedings - IEEE Symposium on Computer-Based Medical Systems · doi:10.1109/cbms65348.2025.00057 · Cited by 1

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Reis, M. H., Antunes, D., Martins, I. B. S., & Caffarena, E. R. (2025) · Lecture notes in computer science · doi:10.1007/978-3-032-09336-3_6

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Emon, M. A., Domingo-Fernández, D., Hoyt, C. T., & Hofmann‐Apitius, M. (2020) · Figshare · doi:10.6084/m9.figshare.12441401

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Thanushiyan, V. (2025) · Sri Lanka Journal of Siddha Medicine · doi:10.65714/sljsm251101

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Haubrich, J. (2021) · theses.fr (ABES) · doi:10.70675/c0d4325dz6fbfz4134z9767z2efed34211f3

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Tyagi, M., Poongavanam, V., Zich, S., Lindhagen, M., Asproudis, I., Putra, O. D., Yang, J., Ashworth, Z. J. R., Guadagni, A., Hagemeyer, L. J., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00830

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Aburayan, W. S., Alradwan, I. A., Alsaffar, B., Alhazzaa, O. A., Almughem, F. A., Alshehri, A. A., Alduhaymi, I. S., Fallatah, M., Alturki, M., Alshaya, H. A., et al. (2026) · Pharmaceutics · doi:10.3390/pharmaceutics18101208

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BindingDB (2023) · UC San Diego · doi:10.7270/q24j0k63

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BindingDB (2024) · UC San Diego · doi:10.7270/q2m90f2k

BindingDB Entry 7930: In silico design of novel probes for the atypical opioid receptor MRGPRX2.

BindingDB (2017) · UC San Diego · doi:10.7270/q20r9n82

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BindingDB (2022) · UC San Diego · doi:10.7270/q2gq72gz

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Wei, L., & Ni, X. (2026) · Journal of Translational Genetics and Genomics · doi:10.20517/jtgg.2026.56

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Rask-Andersen, M., Almén, M. S., & Schiöth, H. B. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3478 · Cited by 853

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Zheng, C. J., Han, L., Yap, C. W., Xie, B., & Chen, Y. (2005) · Drug News & Perspectives · doi:10.1358/dnp.2005.18.2.886480 · Cited by 14

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Liu, X., Zhu, F., Ma, X., Tao, L., Zhang, J., Yang, S., Wei, Y., & Chen, Y. (2011) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.2011.586635 · Cited by 24

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Halip, L., Avram, S. I., Overington, J. P., Al‐Lazikani, B., Curpan, R. F., Sirimulla, S., Pushechnikov, A. O., Beccari, A. R., Savchuk, N., & Oprea, T. I. (2026) · Nature Reviews Drug Discovery · doi:10.1038/s41573-026-01530-3

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Yang, H. J., Yu, C., Li, Y., & Zhu, F. (2017) · Journal of Biosciences and Medicines · doi:10.4236/jbm.2017.53001