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Discovery of N-((3 R,4 R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1 H-pyrazol-4-yl)amino)-9-methyl-9 H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
Abstract
Mutant epidermal growth factor receptor (EGFR) is a major driver of non-small-cell lung cancer (NSCLC). Marketed first generation inhibitors, such as erlotinib, effect a transient beneficial response in EGFR mutant NSCLC patients before resistance mechanisms render these inhibitors ineffective. Secondary oncogenic EGFR mutations account for approximately 50% of relapses, the most common being the gatekeeper T790M substitution that renders existing therapies ineffective. The discovery of PF-06459988 (1), an irreversible pyrrolopyrimidine inhibitor of EGFR T790M mutants, was recently disclosed.1 Herein, we describe our continued efforts to achieve potency across EGFR oncogenic mutations and improved kinome selectivity, resulting in the discovery of clinical candidate PF-06747775 (21), which provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties. Compound 21 is currently being evaluated in phase-I clinical trials of mutant EGFR driven NSCLC.
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“Mavelertinib (PF-06747775) (67) is an orally available and irreversible EGFR TKI that selectively targets various EGFR mutants, such as Del, L858R, T790M/L858R and T790M/Del, with less than 50% effect or inhibition against all nonkinase targets.”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [196]
Citations
Cites
Understanding organofluorine chemistry. An introduction to the C–F bond
O’Hagan, D. (2007) · Chemical Society Reviews · doi:10.1039/b711844a · Cited by 4,128
Epidermal growth factor receptor mutations in lung cancer
Sharma, S. V., Bell, D. W., Settleman, J., & Haber, D. A. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2088 · Cited by 3,170
The resurgence of covalent drugs
Singh, J., Petter, R. C., Baillie, T. A., & Whitty, A. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3410 · Cited by 1,873
A Medicinal Chemist’s Guide to Molecular Interactions
Bissantz, C., Kuhn, B., & Ståhl, M. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm100112j · Cited by 1,810
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Zhou, W., Ercan, D., Chen, L., Yun, C.-H., Li, D., Capelletti, M., Cortot, A. B., Chirieac, L., Iacob, R. E., Padera, R., et al. (2009) · Nature · doi:10.1038/nature08622 · Cited by 1,013
Engelman, J. A., Zejnullahu, K., Gale, C.-M., Lifshits, E., Gonzales, A. J., Shimamura, T., Zhao, F., Vincent, P. W., Naumov, G. N., Bradner, J. E., et al. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-1885 · Cited by 730
Understanding resistance to EGFR inhibitors—impact on future treatment strategies
Wheeler, D. L., Dunn, E. F., & Harari, P. M. (2010) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2010.97 · Cited by 683
Finlay, M. R. V., Anderton, M., Ashton, S., Ballard, P., Bethel, P. A., Box, M. R., Bradbury, R. H., Brown, S. J., Butterworth, S., Campbell, A., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500973a · Cited by 636
Concise review of the glutathione S-transferases and their significance to toxicology
Eaton, D. L. (1999) · Toxicological Sciences · doi:10.1093/toxsci/49.2.156 · Cited by 627
Johnson, T. W., Richardson, P., Bailey, S., Brooun, A., Burke, B. J., Collins, M. R., Cui, J. J., Deal, J. G., Deng, Y., Dinh, D. M., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500261q · Cited by 621
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- 10.1073/pnas.1313733111 · DOI · Paper page
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Sorted by citations
Wu, S., & Shih, J. (2018) · Molecular Cancer · doi:10.1186/s12943-018-0777-1 · Cited by 802
Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396
Lipophilic Efficiency as an Important Metric in Drug Design
Johnson, T. W., Gallego, R. A., & Edwards, M. P. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00077 · Cited by 385
Self-citationAyati, A., Moghimi, S., Salarinejad, S., Safavi, M., Pouramiri, B., & Foroumadi, A. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.103811 · Cited by 394
Third generation EGFR TKIs: current data and future directions
Tan, C., Kumarakulasinghe, N. B., Huang, Y., Ang, Y. L. E., Choo, J. R.-E., Goh, B.-C., & Soo, R. A. (2018) · Molecular Cancer · doi:10.1186/s12943-018-0778-0 · Cited by 322
Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer
Bar-Peled, L., Kemper, E. K., Suciu, R. M., Vinogradova, E. V., Backus, K. M., Horning, B. D., Paul, T. A., Ichu, T.-A., Svensson, R. U., Olucha, J., et al. (2017) · Cell · doi:10.1016/j.cell.2017.08.051 · Cited by 262
Gelatti, A., Drilon, A. E. D. C., & Santini, F. C. (2019) · Lung Cancer · doi:10.1016/j.lungcan.2019.09.017 · Cited by 220
Nagasaka, M., Zhu, V. W., Lim, S. M., Greco, M., Wu, F., & Ou, S.-H. I. (2021) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2020.11.028 · Cited by 219
Fang, H., Peng, B., Ong, S. Y., Wu, Q., Li, L., & Yao, S. Q. (2021) · Chemical Science · doi:10.1039/d1sc01359a · Cited by 215
Progress with covalent small-molecule kinase inhibitors
Zhao, Z., & Bourne, P. E. (2018) · Drug Discovery Today · doi:10.1016/j.drudis.2018.01.035 · Cited by 203
Where Do Recent Small Molecule Clinical Development Candidates Come From?
Brown, D. G., & Boström, J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00675 · Cited by 182
Lu, X., Yu, L., Zhang, Z., Ren, X., Smaill, J. B., & Ding, K. (2018) · Medicinal Research Reviews · doi:10.1002/med.21488 · Cited by 173
Chen, L., Fu, W., Zheng, L., Liu, Z., & Liang, G. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01310 · Cited by 169
Assessing Lysine and Cysteine Reactivities for Designing Targeted Covalent Kinase Inhibitors
Liu, R., Yue, Z., Tsai, C.-C., & Shen, J. (2019) · Journal of the American Chemical Society · doi:10.1021/jacs.8b13248 · Cited by 139
Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitors
Singh, M., & Jadhav, H. R. (2017) · Drug Discovery Today · doi:10.1016/j.drudis.2017.10.004 · Cited by 131
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations
Young, R. J., & Leeson, P. D. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00180 · Cited by 113
Nițulescu, G. M., Stancov, G., Șeremet, O. C., Nițulescu, G., Mihai, D. P., Duta-Bratu, C.-G., Bărbuceanu, Ș., & Olaru, O. T. (2023) · Molecules · doi:10.3390/molecules28145359 · Cited by 108
Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors
Niessen, S., Dix, M. M., Barbas, S., Potter, Z. E., Lu, S., Brodsky, O., Planken, S., Behenna, D. C., Almaden, C., Gajiwala, K. S., et al. (2017) · Cell chemical biology · doi:10.1016/j.chembiol.2017.08.017 · Cited by 99
Self-citationWright, N. A., & Goss, G. D. (2019) · Translational Lung Cancer Research · doi:10.21037/tlcr.2019.06.01 · Cited by 95
RamPlot : a webserver to draw 2D, 3D and assorted Ramachandran (φ, ψ) maps
Kumar, M., & Rathore, R. S. (2025) · Journal of Applied Crystallography · doi:10.1107/s1600576725001669 · Cited by 76
Iorkula, T. H., Osayawe, O. J.-K., Odogwu, D. A., Ganiyu, L. O., Faderin, E., Awoyemi, R. F., Akodu, B. O., Ifijen, I. H., Aworinde, O. R., Agyemang, P., et al. (2025) · RSC Advances · doi:10.1039/d4ra07556k · Cited by 70
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Borsari, C., Keleş, E., McPhail, J. A., Schäfer, A., Sriramaratnam, R., Goch, W., Schaefer, T., Pascale, M. D., Bal, W., Gstaiger, M., et al. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.1c13568 · Cited by 65
Li, J., Guan, X., Zhang, O., Sun, K., Wang, Y., Bagni, D., & Head-Gordon, T. L. (2026) · The Journal of Physical Chemistry B · doi:10.1021/acs.jpcb.5c08598 · Cited by 57
Self-citationNiggenaber, J., Heyden, L., Grabe, T., Müller, M. P., Lategahn, J., & Rauh, D. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00472 · Cited by 57
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Zhang, H., Wang, J., Shen, Y. H., Wang, H., Duan, W.-M., Zhao, H., Hei, Y., Xin, M., Cao, Y., & Zhang, S. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.02.051 · Cited by 54
Dhameliya, T. M., Patel, K. I., Tiwari, R., Vagolu, S. K., Panda, D., Sriram, D., & Chakraborti, A. K. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.104538 · Cited by 47
The role of quantum chemistry in covalent inhibitor design
Mihalovits, L. M., Ferenczy, G. G., & Keserű, G. M. (2021) · International Journal of Quantum Chemistry · doi:10.1002/qua.26768 · Cited by 46
Ahmad, I., Shaikh, M., Surana, S. J., Ghosh, A., & Patel, H. (2020) · Journal of Biomolecular Structure and Dynamics · doi:10.1080/07391102.2020.1844801 · Cited by 44
Shrestha, R. M., Mahiya, K., Shrestha, A., Mohanty, S. R., Yadav, S. K., & Yadav, P. N. (2023) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2023.136945 · Cited by 44
Shrestha, R. M., Mahiya, K., Shrestha, A., Mohanty, S. R., Yadav, S. K., & Yadav, P. N. (2024) · Inorganic Chemistry Communications · doi:10.1016/j.inoche.2024.112142 · Cited by 41
Wang, L., Zhao, J., Yao, Y., Wang, C., Zhang, J., Shu, X. H., Sun, X., Li, Y., Liu, K., Yuan, H., et al. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.09.024 · Cited by 39
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Sato, M., Fuchida, H., Shindo, N., Kuwata, K., Tokunaga, K., Xiao-Lin, G., Inamori, R., Hosokawa, K., Watari, K., Shibata, T., et al. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00574 · Cited by 38
Xiao, Z., Zhou, Z., Chu, C., Zhang, Q., Zhou, L., Yang, Z., Li, X., Yu, L., Zheng, P., Xu, S., et al. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112511 · Cited by 36
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Abdelbaky, I., Tayara, H., & Chong, K. T. (2021) · Scientific Reports · doi:10.1038/s41598-020-80758-4 · Cited by 35
Das, D., Wang, J., & Hong, J. (2021) · ChemMedChem · doi:10.1002/cmdc.202100166 · Cited by 35
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Wang, H.-T., Wang, Y., Liu, S., Mai, Y., Zong, X., Gao, H., Hu, R., Jiang, X., & Yeung, Y. (2019) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201900814 · Cited by 32
Self-citationPoels, K. E., Schoenfeld, A. J., Makhnin, A., Tobi, Y. Y., Wang, Y., Cabanos, H. F., Chakrabarti, S., Shi, M., Napoli, C., McDonald, T. O., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-23912-4 · Cited by 32
Self-citationChen, D., Guo, D., Yan, Z., & Zhao, Y. (2017) · MedChemComm · doi:10.1039/c7md00571g · Cited by 32
Gawli, C., Patil, C. R., & Patel, H. (2025) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2025.118146 · Cited by 27
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Xiao, Z., Chu, C., Zhou, L., Zhou, Z., Zhang, Q., Yang, F., Yang, Z., Zheng, P., Xu, S., & Zhu, W. (2020) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2020.115669 · Cited by 27
Todsaporn, D., Zubenko, A. A., Kartsev, V. G., Aiebchun, T., Mahalapbutr, P., Petrou, A., Geronikaki, A. A., Диваева, Л. Н., Chekrisheva, V., Yıldız, İ., et al. (2023) · Molecules · doi:10.3390/molecules28073014 · Cited by 28
Li, W., Zhang, J., Wang, M., Dong, R., Zhou, X., Zheng, X. X., & Sun, L. (2022) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026622666220111143949 · Cited by 25
Li, S., Zhu, S., Wei, H., Zhu, P., Jiao, Y., Yi, M., Gong, J., Zheng, K., & Zhang, L. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.113959 · Cited by 26
Chen, L., Fu, W., Feng, C., Qu, R., Tong, L., Zheng, L., Fang, B., Qiu, Y., Hu, J., Cai, Y., et al. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.08.061 · Cited by 24
Chen, Y., Yang, L., Qiao, H., Cheng, Z., Xie, J., Zhou, W., Huang, X., Jiang, Y., Yu, B., & Zhao, W. H. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112388 · Cited by 24
Gong, Y., Wu, F., Wang, M., Xu, H.-C., Zhuo, L., Yang, G., & Huang, W. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114654 · Cited by 22
Zhang, H., Wang, J., Zhao, H., Yang, X., Lei, H., Xin, M., Cao, Y., & Zhang, S. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.05.039 · Cited by 22
Bijian, K., Wernic, D., Nivedha, A. K., Su, J., Lim, F. P. L., Miron, C. E., Amzil, H., Moitessier, N., & Alaoui‐Jamali, M. A. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01031 · Cited by 21
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Franovic, A., Raymond, V. M., Erlander, M. G., & Reckamp, K. L. (2017) · Journal of Thoracic Disease · doi:10.21037/jtd.2017.06.144 · Cited by 20
Lü, X., Wu, Y., Yang, J., Ma, F.-E., Li, L., Chen, S., Zhang, Y., Ni, Q., Pan, Y., Hong, X., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.074 · Cited by 19
Liu, J., Zhang, C., Liu, S., Wang, X., Wu, X.-Z., & Hao, J. (2022) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-022-02316-1 · Cited by 16
Self-citationGan, W., Wang, C., Pan, Q., Li, Y., Guo, Y., Fan, D., Peng, Y., Rao, Z., Xu, S., Zheng, P., et al. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.105994 · Cited by 15
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Chevis, P. J., Wangngae, S., Thaima, T., Carroll, A. W., Willis, A. C., Pattarawarapan, M., & Pyne, S. G. (2019) · Chemical Communications · doi:10.1039/c9cc02765c · Cited by 15
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Tan, A. C., Teh, Y. L., Lai, G. G. Y., & Tan, D. S.-W. (2019) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2019.1604228 · Cited by 15
Lucas, S. C. C., Milbradt, A. G., Blackwell, J. H., Bonomo, S., Brierley, A., Cassar, D. J., Freeman, J., Hadfield, T. E., Morrill, L. A., Riemens, R., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00781 · Cited by 15
Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies
Damghani, T., Chitnis, S. P., Abidakun, O. A., Patel, K. B., Lin, K. S., Ouellette, E. A., Lantry, A. M., & Heppner, D. E. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01661 · Cited by 13
Kakarala, K. K., & Jamil, K. (2021) · Journal of Biomolecular Structure and Dynamics · doi:10.1080/07391102.2021.1891140 · Cited by 13
Hajjo, R., Sabbah, D. A., Bardaweel, S. K., & Zhong, H. A. (2024) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2024.2327307 · Cited by 14
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Michaels, S. A., Hulverson, M. A., Whitman, G. R., Tran, L. T. N., Choi, R., Fan, E., McNamara, C. W., Love, M. S., & Ojo, K. K. (2022) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00017-22 · Cited by 11
Mao, L., Tang, W., Zhang, X., Liu, J., Chen, Y., Hua, Y., Weng, B., Mo, X., Bao, Y., Li, T., et al. (2020) · Medicine in Drug Discovery · doi:10.1016/j.medidd.2020.100035 · Cited by 11
Cho, B. C., Goldberg, S. B., Kim, D., Socinski, M. A., Burns, T. F., Lwin, Z., Pathan, N., Wei, D., Masters, J. C., Cossons, N., et al. (2022) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2022.2075341 · Cited by 10
Widlicka, D. W., Gontcharov, A. V., Mehta, R., Pedro, D. J., & North, R. (2019) · Organic Process Research & Development · doi:10.1021/acs.oprd.9b00245 · Cited by 10
Wang, T., Gao, Y., Wu, F., Luo, L., Ma, J., & Hu, Y. (2024) · RSC Medicinal Chemistry · doi:10.1039/d3md00668a · Cited by 9
Origami with small molecules: exploiting the C–F bond as a conformational tool
Ryan, P., Iftikhar, R., & Hunter, L. (2025) · Beilstein Journal of Organic Chemistry · doi:10.3762/bjoc.21.54 · Cited by 9
Prospect of reprogramming replication licensing for cancer drug development
Kyei-Barffour, I., & Acheampong, D. O. (2021) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2020.111190 · Cited by 9
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors
Mansour, T. S., Potluri, V. K., Pallepati, R., Basetti, V., Keesara, M., Moghudula, A. G., & Maiti, P. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.04.029 · Cited by 8
Ren, J., Dai, J., Chen, Y., Wang, Z., Sha, R., Mao, J., & Mao, Y. (2024) · Metabolites · doi:10.3390/metabo14040224 · Cited by 7
Yogesh, H. S., Shaik, S. F., Sangi, S., Swaroop, K., Sreeharsha, N., Anitha, K. N., Mishra, V. K., Kurmi, S. P. C., Nath, S., & Thapa, S. (2025) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-025-04690-y · Cited by 6
Feng, Y.-Y., Liu, J.-F., Xue, Y., Liu, D., & Wu, X.-Z. (2024) · Chinese Journal of Integrative Medicine · doi:10.1007/s11655-024-3717-5 · Cited by 6
Hu, G., Xu, H., Yang, W., Hao, A., Sun, W., Shen, W., & Hu, Y. (2021) · The Journal of Chemical Thermodynamics · doi:10.1016/j.jct.2021.106493 · Cited by 6
Konsue, A., Lamtha, T., Gleeson, D., Jones, D. J. L., Britton, R. G., Pickering, J., Choowongkomon, K., & Gleeson, M. P. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117906 · Cited by 5
Zhu, T.-F., Qian, R., Wei, X., Lü, A., & Cao, D. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01893 · Cited by 5
Akher, F. B., Farrokhzadeh, A., Ravenscroft, N., & Kuttel, M. M. (2019) · Biochemistry · doi:10.1021/acs.biochem.9b00710 · Cited by 5
In Silicon Approach for Discovery of Chemopreventive Agents
Wang, J., Li, W., Wang, B., Hu, B., Jiang, H., Lai, B., Li, N., & Cheng, M. (2017) · Current Pharmacology Reports · doi:10.1007/s40495-017-0094-1 · Cited by 4
Shvetsov, A. B., & Semenov, A. (2024) · Russian Journal of Bioorganic Chemistry · doi:10.1134/s1068162024060347 · Cited by 3
Mohamed, M. A., Ali, A., Ali, A., Afzal, O., Ahsan, M. F., Alamri, M. A., Alossaimi, M. A., Altamimi, A. S. A., Salahuddin, S., & Ahsan, M. J. (2024) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2024.138826 · Cited by 3
Kageji, H., Momose, T., Ebisawa, M., Nakazawa, Y., OKADA, H. M., Togashi, N., Nagamoto, Y., Obuchi, W., Yasumatsu, I., Kihara, K., et al. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117862 · Cited by 2
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Hooper, A. R., & Burns, A. S. (2022) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.2c00075 · Cited by 2
Lahiani, A., Haham, D., Lankri, D., Cornell-Kennon, S., Schaefer, E., Tsvelikhovsky, D., & Lazarovici, P. (2020) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.0c00255 · Cited by 2
Schmalhorst, P. S., & Bergner, A. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c00051 · Cited by 2
Karl, K., Light, T. P., & Hristova, K. A. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-820472-6.00135-3 · Cited by 2
Ferreira, L. L. G., & Andricopulo, A. D. (2021) · Wiley eBooks · doi:10.1002/0471266949.bmc141.pub2 · Cited by 2
Jannu, M., Vankadoth, U. N., Umamaheswari, A., & Jinka, R. (2025) · Journal of Receptors and Signal Transduction · doi:10.1080/10799893.2025.2590462 · Cited by 1
Karati, D., Sen, D., Mahanti, B., Roy, S., & Mukherjee, S. (2026) · Discover Chemistry. · doi:10.1007/s44371-026-00503-0 · Cited by 1
Pal, S., & Mohanty, D. (2026) · Computational and Structural Biotechnology Journal · doi:10.34133/csbj.0118 · Cited by 1
Shvetsov, A. B., & Semenov, A. V. (2024) · Биоорганическая химия · doi:10.31857/s0132342324060037
Boras, B. W., Greenwald, E. C., Wang, Y., Shi, M., Pascual, B., Cianfrogna, J. A., Bartlett, D. W., & Spilker, M. E. (2025) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-025-09986-3
Self-citationAhsan, M. F., Ahsan, M. J., Yusuf, M., Syed, T., Asiri, Y. I., Ali, A., & Salahuddin, S. (2025) · Journal of Taibah University for Science · doi:10.1080/16583655.2025.2544430
Pal, S., & Mohanty, D. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2025.12.01.691623
Setiawan, D., Hadi, S., Mahdi, N. I., Mardiati, N., Sutomo, Rizki, M. I., Normaidah, N., Buih, P. H. J., Nugraha, A. T., Apriliany, F., et al. (2026) · Journal of Applied Pharmaceutical Science · doi:10.1177/22313354261461005
Munir, F., Hussain, K., Zhao, G., & Zhang, J. (2026) · Computer Methods and Programs in Biomedicine · doi:10.1016/j.cmpb.2026.109679
Dahab, M. A., Ashoub, A. F., Ali, R. A., Sallam, A. S., & Mayhoub, A. S. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.119449
BindingDB Entry 50013322: Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR
BindingDB (2022) · UC San Diego · doi:10.7270/q24x5cjs
BindingDB (2020) · UC San Diego · doi:10.7270/q2dj5j62
BindingDB (2022) · UC San Diego · doi:10.7270/q2736vnz
BindingDB Entry 50001188: Lipophilic Efficiency as an Important Metric in Drug Design.
BindingDB (2020) · UC San Diego · doi:10.7270/q2wm1gwq
Metadata
- Authors
- Planken, S., Behenna, D. C., Nair, S. K., Johnson, T. O., Nagata, A., Almaden, C., Bailey, S., Ballard, T. E., Bernier, L., Cheng, H., Cho-Schultz, S., Dalvie, D., Deal, J. G., Dinh, D. M., Edwards, M. P., Ferre, R. A., Gajiwala, K. S., Hemkens, M., Kania, R. S., Kath, J. C., Matthews, J., Murray, B. W., Niessen, S., Orr, S. T. M., Pairish, M., Sach, N. W., Shen, H., Shi, M., Solowiej, J., Tran, K., Tseng, E., Vicini, P., Wang, Y., Weinrich, S. L., Zhou, R., Zientek, M., Liu, L., Luo, Y., Xin, S., Zhang, C., & Lafontaine, J.
- Affiliations
- Pfizer (United States) (US)
- WuXi AppTec (China) (CN)
- Corresponding author
- Planken, Simon
- Behenna, Douglas C.
- ORCID
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2017-03-29
- Volume
- 60
- Issue
- 7
- Pages
- 3002-3019
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2597231917
- Cited by
- 97
- References
- 44
- Citations by year
- 2026: 8 · 2025: 12 · 2024: 12 · 2023: 5 · 2022: 10 · 2021: 10 · 2020: 12 · 2019: 9 · 2018: 10 · 2017: 9
- FWCI
- 10.40
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Keywords
- EGFR inhibitors, T790M mutation, non-small cell lung cancer, irreversible kinase inhibitors, structure-based drug design, pyrrolopyrimidine, exon 19 deletion, L858R mutation, gatekeeper mutation, kinase selectivity, ADME properties, erlotinib resistance
- MeSH terms
- Acrylamides, Animals, Carcinoma, Non-Small-Cell Lung, Dogs, Humans, Lung, Lung Neoplasms, Models, Molecular, Mutation, Pyrrolidines, Drug Design, Cell Line, Tumor, Protein Kinase Inhibitors, Mice, Rats, Halogenation, Molecular Docking Simulation, ErbB Receptors
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