Table 1. KRasG12C switch-II pocket inhibitors.
Compound name in publication | Numbering in this article | Chemical structure | PDB ID | Reference | Company/origin | Phase | ID |
2E07 | 1 | — | Ostrem et al. (2013)22 | Shokat Laboratory | — | — | |
6H05 | 2 | — | Ostrem et al. (2013)22 | Shokat Laboratory | — | — | |
Compound 6 | 3 | 4luc | Ostrem et al. (2013)22 | Shokat Laboratory | — | — | |
Compound 9 | 4 | 4lyh | Ostrem et al. (2013)22 | Shokat Laboratory | — | — | |
4lyj | |||||||
Compound 12 | 5 | — | Ostrem et al. (2013)22 | Shokat Laboratory | — | — | |
ARS-107 | 6 | 6b0v | Patricelli et al. (2016)23 | Wellspring Bioscience | — | — | |
ARS-853 | 7 | 5f2e | Patricelli et al. (2016)23 | Wellspring Bioscience | — | — | |
ARS-1620 | 8 | 5v9u | Janes et al. (2018)24 | Wellspring Bioscience | — | — | |
Indole lead 1 | 9 | 6p8z | Shin et al. (2019)27 | Amgen | — | — | |
AMG 510 | 10 | 6oim | Canon et al. (2019)29 | Amgen | I/II | NCT03600883 | |
NCT04185883 | |||||||
Compound 4 | 11 | 6n2j | Fell et al. (2018)36 | Array BioPharma | — | — | |
Mirati Therapeutics | |||||||
Compound 13 | 12 | — | Fell et al. (2018)36 | Array BioPharma | — | — | |
Mirati Therapeutics | |||||||
MRTX849 | 13 | 6ut0 | Hallin et al. (2019)37 | Mirati Therapeutics | I/II | NCT03785249 | |
Fell et al. (2020)38 | |||||||
JNJ-74699157 (ARS-3248) | 14 | — | — | — | J&J Wellspring Bioscience | I | NCT04006301 |