Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure.

Phillips DP, Alper PB, Borkin D, Han D, Kochanek SE, Gurjar J, Mathison CJN, Nelson JM, Pei W, Nguyen BN, Hoffman T, Okram B, Nguyen TN, Jiang S, Masick BT, Wang Z, Cho CY, Yin H, Chen Y, Juarez J, Jia Y, Zhou V, Liu G, Wright C, Nguyen T, Knee DA, Liu Q, Liu J, Li J, Virata C, de Oliveira C, DiDonato M, Bursulaya B, Vidal-Biggart A, Jones DH, Witmer D, Chu C, Jin H, Herath A, Richmond W, Groessl T, Shapiro M, Effenberger K, Arroyo K, Bretz A, Honda A, Gordon WP, Molteni V, Haling JR

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DOI: 10.1021/acs.jmedchem.6c01454
Published: 2026 Sep 10
Container: Journal of medicinal chemistry
Publisher: Not recorded
Open access: unknown

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Cite this work

BibTeX

@article{allodium:10.1021/acs.jmedchem.6c01454,
  title = {Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure.},
  author = {Phillips DP and Alper PB and Borkin D and Han D and Kochanek SE and Gurjar J and Mathison CJN and Nelson JM and Pei W and Nguyen BN and Hoffman T and Okram B and Nguyen TN and Jiang S and Masick BT and Wang Z and Cho CY and Yin H and Chen Y and Juarez J and Jia Y and Zhou V and Liu G and Wright C and Nguyen T and Knee DA and Liu Q and Liu J and Li J and Virata C and de Oliveira C and DiDonato M and Bursulaya B and Vidal-Biggart A and Jones DH and Witmer D and Chu C and Jin H and Herath A and Richmond W and Groessl T and Shapiro M and Effenberger K and Arroyo K and Bretz A and Honda A and Gordon WP and Molteni V and Haling JR},
  year = {2026},
  journal = {Journal of medicinal chemistry},
  doi = {10.1021/acs.jmedchem.6c01454},
  url = {https://doi.org/10.1021/acs.jmedchem.6c01454}
}

RIS

TY  - JOUR
TI  - Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure.
AU  - Phillips DP
AU  - Alper PB
AU  - Borkin D
AU  - Han D
AU  - Kochanek SE
AU  - Gurjar J
AU  - Mathison CJN
AU  - Nelson JM
AU  - Pei W
AU  - Nguyen BN
AU  - Hoffman T
AU  - Okram B
AU  - Nguyen TN
AU  - Jiang S
AU  - Masick BT
AU  - Wang Z
AU  - Cho CY
AU  - Yin H
AU  - Chen Y
AU  - Juarez J
AU  - Jia Y
AU  - Zhou V
AU  - Liu G
AU  - Wright C
AU  - Nguyen T
AU  - Knee DA
AU  - Liu Q
AU  - Liu J
AU  - Li J
AU  - Virata C
AU  - de Oliveira C
AU  - DiDonato M
AU  - Bursulaya B
AU  - Vidal-Biggart A
AU  - Jones DH
AU  - Witmer D
AU  - Chu C
AU  - Jin H
AU  - Herath A
AU  - Richmond W
AU  - Groessl T
AU  - Shapiro M
AU  - Effenberger K
AU  - Arroyo K
AU  - Bretz A
AU  - Honda A
AU  - Gordon WP
AU  - Molteni V
AU  - Haling JR
PY  - 2026
JO  - Journal of medicinal chemistry
DO  - 10.1021/acs.jmedchem.6c01454
UR  - https://doi.org/10.1021/acs.jmedchem.6c01454
ER  -

APA

DP, P., PB, A., D, B., D, H., SE, K., J, G., CJN, M., JM, N., W, P., BN, N., T, H., B, O., TN, N., S, J., BT, M., Z, W., CY, C., H, Y., Y, C., J, J., Y, J., V, Z., G, L., C, W., T, N., DA, K., Q, L., J, L., J, L., C, V., C, D. O., M, D., B, B., A, V., DH, J., D, W., C, C., H, J., A, H., W, R., T, G., M, S., K, E., K, A., A, B., A, H., WP, G., V, M., & JR, H. (2026). Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure.. Journal of medicinal chemistry. https://doi.org/10.1021/acs.jmedchem.6c01454

Source records

pubmed · retrieved 2026-09-26T11:49:44.547Z